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Articles
Autophagy in Cancer Promotes Therapeutic Resistance
Autophagy is a highly regulated process by which long-lived proteins, organelles, and protein aggregates are captured within autophagosomes, which are then fused with lysosomes for degradation.1 Auto...
Linda Stephenson, Ph.D., Product Specialist, Sigma® Life Science
Biofiles, Vol. 8, No. 9
Keywords: Apoptosis, Autophagy, Cancer, Degradations, Metabolites, transformation
DNA Damage and Repair
Damage to cellular DNA is involved in mutagenesis and the development of cancer. The DNA in a human cell undergoes several thousand to a million damaging events per day, generated by both external (e...
BioFiles 2007, 2.4, 20.
Keywords: AGE, Alkylations, Apoptosis, Biochemistry, Cancer, Carcinogens, Catalysis, Clinical, DNA replication, Deaminations, Environmental, Gene expression, Metabolites, Methylations, Mutagens, Oxidations, Polymorphisms, Rearrangements, Recombination, Substitutions, Transcription
Nucleotide Synthesis in Cancer Cells
Neoplastic cells are highly dependent on the de novo synthesis of nucleotides to maintain sufficient pools to support DNA replication and the production of RNA. The metabolic pathways supporting nucl...
Keywords: Cancer, Catalysis, DNA replication, Gene expression, Glycolysis, Metabolic Pathways, Metabolism, Metabolites, Nucleotide Synthesis, PAGE, Pentose phosphate pathway, Pyrimidine synthesis
Papers
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Nucleoside-mediated mitigation of 5-fluorouracil-induced toxicity in synchronized murine erythroleukemic cells. Elstein, K.H., et al. Toxicol. Appl. Pharmacol. 146, 29-39, (1997)
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Effect of 5-fluorouracil on cell cycle regulatory proteins in human colon cancer cell line. Takeda, H., et al. Jpn. J. Cancer Res. 90, 677-684, (1999)
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5-FU-induced apoptosis correlates with efficacy against human gastric and colon cancer xenografts in nude mice. Inada, T., et al. Anticancer Res. 17, 1965-1971, (1997)
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Selective Activation Of SHP2 Activity By Cisplatin Revealed By A Novel Chemical Probe-based Assay. Kuo, C.C., et al. Biochem. Biophys. Res. Commun. 391, 230-4, (2010)
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Arcobacter Population Dynamics In Pigs On Farrow-to-Finish Farms. De Smet, S., et al. Appl. Environ. Microbiol. 77, 1732-8, (2011)
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Differential Expression Of The Klf6 Tumor Suppressor Gene Upon Cell Damaging Treatments In Cancer Cells. Gehrau, R.C., et al. Mol. Cell. 707, 15-23, (2011)
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A quantitative trait locus on chromosome 4 affects cycling of hematopoietic stem and progenitor cells through regulation of TGF-β 2 responsiveness. Serine Avagyan et al J. Immunol. 181, 5904-11, (2008)
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Counteracting quasispecies adaptability: extinction of a ribavirin-resistant virus mutant by an alternative mutagenic treatment. Celia Perales et al PLoS ONE 4, e5554, (2009)
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A novel fluorescence-based assay for the rapid detection and quantification of cellular deoxyribonucleoside triphosphates. Peter M. Wilson et al Nucleic Acids Res. 39, e112, (2011)
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Antiproliferative property of hexadecyloxypropyl 9-[2-(phosphonomethoxy) ethyl] guanine (HDP-PMEG) for unwanted ocular proliferation. Jiangping Hou et al Mol. Vis. 17, 627-37, (2011)
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Parallel evolution under chemotherapy pressure in 29 breast cancer cell lines results in dissimilar mechanisms of resistance. Bálint Tegze et al PLoS ONE 7, e30804, (2012)
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Discovery of 2-arylthiazolidine-4-carboxylic acid amides as a new class of cytotoxic agents for prostate cancer. Veeresa Gududuru et al J. Med. Chem. 48, 2584-8, (2005)
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Antitumor-active cobalt-alkyne complexes derived from acetylsalicylic acid: studies on the mode of drug action. Ingo Ott et al J. Med. Chem. 48, 622-9, (2005)
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Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. Heyong Gao et al Bioorg. Med. Chem. Lett. 15, 2003-6, (2005)
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Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. Heyong Gao et al Bioorg. Med. Chem. Lett. 15, 3233-6, (2005)
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SAR studies of 2-arylthiazolidine-4-carboxylic acid amides: a novel class of cytotoxic agents for prostate cancer. Veeresa Gududuru et al Bioorg. Med. Chem. Lett. 15, 4010-3, (2005)
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Constituents of the pericarp of Garcinia subelliptica. Chien-Chang Wu et al J. Nat. Prod. 68, 1125-7, (2005)
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Cytotoxic prenylflavonoids from Artocarpus elasticus. Horng-Huey Ko et al J. Nat. Prod. 68, 1692-5, (2005)
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Discovery of antiglioma activity of biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues. Michael L Mohler et al J. Med. Chem. 49, 5845-8, (2006)
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Synthesis and biological activities of nucleoside-estradiol conjugates. Hasrat Ali et al Bioorg. Med. Chem. Lett. 16, 317-9, (2006)
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Synthesis, aerobic cytotoxicity, and radiosensitizing activity of novel 2,4-dinitrophenylamine tethered 5-fluorouracil and hydroxyurea. Ali Khalaj et al Bioorg. Med. Chem. Lett. 16, 6034-8, (2006)
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Fish venom (Pterios volitans) peptide reduces tumor burden and ameliorates oxidative stress in Ehrlich's ascites carcinoma xenografted mice. M Sri Balasubashini et al Bioorg. Med. Chem. Lett. 16, 6219-25, (2006)
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Study on synthesis and biological activity of a galactosylated piperazinyl porphyrin. He-Ping Li et al Bioorg. Med. Chem. Lett. 16, 6298-301, (2006)
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Gymnastatins F-H, cytostatic metabolites from the sponge-derived fungus Gymnascella dankaliensis. Taro Amagata et al J. Nat. Prod. 69, 1384-8, (2006)
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Bioactive triterpene glycosides from the sea cucumber Holothuria fuscocinerea. Shu-Yu Zhang et al J. Nat. Prod. 69, 1492-5, (2006)
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Bromophenols coupled with methyl gamma-ureidobutyrate and bromophenol sulfates from the red alga Rhodomela confervoides. Ming Ma et al J. Nat. Prod. 69, 206-10, (2006)
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Flavan-4-ol Glycosides from the Rhizomes of Abacopteris penangiana. Zhongxiang Zhao et al J. Nat. Prod. 69, 265-8, (2006)
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Antineoplastic agents. 551. Isolation and structures of bauhiniastatins 1-4 from Bauhinia purpurea. George R Pettit et al J. Nat. Prod. 69, 323-7, (2006)
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Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Strom, E., et al. Nat. Chem. Biol. 2, 474-479, (2006)
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Probing the anticancer activity of nucleoside analogues: a QSAR model approach using an internally consistent training set. Aliuska Morales Helguera et al J. Med. Chem. 50, 1537-45, (2007)
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Scaffold targeting drug-resistant colon cancers. Katerina Otrubova et al J. Med. Chem. 50, 1999-2002, (2007)
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Synthesis and cytotoxic activity of 17-carboxylic acid modified 23-hydroxy betulinic acid ester derivatives. Yi Bi et al Bioorg. Med. Chem. Lett. 17, 1475-8, (2007)
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Cytotoxic and apoptotic activities of novel amino analogues of boswellic acids. Bhahwal A Shah et al Bioorg. Med. Chem. Lett. 17, 6411-6, (2007)
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Efficient synthesis and in vitro cytostatic activity of 4-substituted triazolyl-nucleosides. Khalid El Akri et al Bioorg. Med. Chem. Lett. 17, 6656-9, (2007)
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Synthesis and biological activities of novel dexibuprofen tetraacetylriboflavin conjugates. Christian Banekovich et al Bioorg. Med. Chem. Lett. 17, 683-7, (2007)
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Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents. Maojiang Wu et al Bioorg. Med. Chem. Lett. 17, 869-73, (2007)
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5-Alkynyl-2'-deoxyuridines: chromatography-free synthesis and cytotoxicity evaluation against human breast cancer cells. Srinivasarao Meneni et al Bioorg. Med. Chem. 15, 3082-8, (2007)
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An efficient synthesis of 3-fluoro-5-thio-xylofuranosyl nucleosides of thymine, uracil, and 5-fluorouracil as potential antitumor or/and antiviral agents. Evangelia Tsoukala et al Bioorg. Med. Chem. 15, 3241-7, (2007)
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2,3,5-Substituted tetrahydrofurans as cancer chemopreventives. Part 1: synthesis and anti-cancer activities of 5-hydroxymethyl-2,3-diaryl-tetrahydro-furan-3-ols. Palwinder Singh et al Bioorg. Med. Chem. 15, 3990-6, (2007)
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Design, syntheses, and antitumor activity of novel chromone and aurone derivatives. Wei Huang et al Bioorg. Med. Chem. 15, 5191-7, (2007)
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Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. George Agelis et al Bioorg. Med. Chem. 15, 5448-56, (2007)
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Synthesis and antiproliferative activity of clausine E, mukonine, and koenoline bioisosteres. François Liger et al Bioorg. Med. Chem. 15, 5615-9, (2007)
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Characterized mechanism of alpha-mangostin-induced cell death: caspase-independent apoptosis with release of endonuclease-G from mitochondria and increased miR-143 expression in human colorectal cancer DLD-1 cells. Yoshihito Nakagawa et al Bioorg. Med. Chem. 15, 5620-8, (2007)
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E,E,E-1-(4-Arylamino-4-oxo-2-butenoyl)-3,5-bis(arylidene)-4-piperidones: a topographical study of some novel potent cytotoxins. Amitabh Jha et al Bioorg. Med. Chem. 15, 5854-65, (2007)
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Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds. Bram Baert et al Bioorg. Med. Chem. 15, 6943-55, (2007)
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Solvatochromism, DNA binding, antitumor activity and molecular modeling study of mixed-ligand copper(II) complexes containing the bulky ligand: bis[N-(p-tolyl)imino]acenaphthene. Usama El-Ayaan et al Eur. J. Med. Chem. 42, 1325-33, (2007)
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Synthesis and cytotoxic evaluation of a series of resveratrol derivatives modified in C2 position. Xian-Feng Huang et al Eur. J. Med. Chem. 42, 263-7, (2007)
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Novel and versatile methodology for synthesis of cyclic imides and evaluation of their cytotoxic, DNA binding, apoptotic inducing activities and molecular modeling study. Alaa A-M Abdel-Aziz et al Eur. J. Med. Chem. 42, 614-26, (2007)
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Synthetic 2',5'-dimethoxychalcones as G(2)/M arrest-mediated apoptosis-inducing agents and inhibitors of nitric oxide production in rat macrophages. Bai-Luh Wei et al Eur. J. Med. Chem. 42, 660-8, (2007)
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Design, synthesis and cytotoxic properties of novel 1-[4-(2-alkylaminoethoxy)phenylcarbonyl]-3,5-bis(arylidene)-4-piperidones and related compounds. Umashankar Das et al Eur. J. Med. Chem. 42, 71-80, (2007)
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Synthetic studies on novel benzimidazolopeptides with antimicrobial, cytotoxic and anthelmintic potential. Rajiv Dahiya et al Eur. J. Med. Chem. 42, 772-98, (2007)
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Molecular mechanism of flucytosine resistance in Candida lusitaniae: contribution of the FCY2, FCY1, and FUR1 genes to 5-fluorouracil and fluconazole cross-resistance. Nicolas Papon et al Antimicrob. Agents Chemother. 51, 369-71, (2007)
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Combination of amphotericin B with flucytosine is active in vitro against flucytosine-resistant isolates of Cryptococcus neoformans. Patrick Schwarz et al Antimicrob. Agents Chemother. 51, 383-5, (2007)
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Stellettins L and M, cytotoxic isomalabaricane-type triterpenes, and sterols from the marine sponge Stelletta tenuis. Hou-wen Lin et al J. Nat. Prod. 70, 1114-7, (2007)
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Cytotoxic benzo[j]fluoranthene metabolites from Hypoxylon truncatum IFB-18, an endophyte of Artemisia annua. W Gu et al J. Nat. Prod. 70, 114-7, (2007)
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Cytotoxic diterpenoids from the bark of Pseudolarix kaempferi and their structure-activity relationships. Peng Liu et al J. Nat. Prod. 70, 533-7, (2007)
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Chemical genetics reveals a complex functional ground state of neural stem cells Diamandis, P., et. al. Nat. Chem. Biol. 3(5), 268-273, (2007)
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Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. Gustav Ahlin et al J. Med. Chem. 51, 5932-42, (2008)
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Synthesis, cytotoxicity, and anti-Trypanosoma cruzi activity of new chalcones. José C Aponte et al J. Med. Chem. 51, 6230-4, (2008)
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Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. Lourdes Santana et al J. Med. Chem. 51, 6740-51, (2008)
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Anticancer activity of (1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl)-pyrimidines and -purines against the MCF-7 cell line: Preliminary cDNA microarray studies. Mónica Díaz-Gavilán et al Bioorg. Med. Chem. Lett. 18, 1457-60, (2008)
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Synthesis and biological evaluation of novel 1-O- and 14-O-derivatives of oridonin as potential anticancer drug candidates. Jinyi Xu et al Bioorg. Med. Chem. Lett. 18, 4741-4, (2008)
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Synthesis and cytotoxic activity of some novel polycyclic gamma-butyrolactones. M P S Ishar et al Bioorg. Med. Chem. Lett. 18, 4809-12, (2008)
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Constituents of Brazilian red propolis and their preferential cytotoxic activity against human pancreatic PANC-1 cancer cell line in nutrient-deprived condition. Suresh Awale et al Bioorg. Med. Chem. 16, 181-9, (2008)
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Cytotoxic constituents from Brazilian red propolis and their structure-activity relationship. Feng Li et al Bioorg. Med. Chem. 16, 5434-40, (2008)
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Synthesis, cytostatic and anti-HIV evaluations of the new unsaturated acyclic C-5 pyrimidine nucleoside analogues. Tatjana Gazivoda et al Bioorg. Med. Chem. 16, 5624-34, (2008)
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Synthesis and antitumor activity evaluations of albumin-binding prodrugs of CC-1065 analog. Yuqiang Wang et al Bioorg. Med. Chem. 16, 6552-9, (2008)
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Synthesis and evaluation of unsymmetrical polyamine derivatives as antitumor agents. Jianhong Wang et al Bioorg. Med. Chem. 16, 7005-12, (2008)
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Synthesis and cytotoxic, anti-inflammatory, and anti-oxidant activities of 2',5'-dialkoxylchalcones as cancer chemopreventive agents. Jen-Hao Cheng et al Bioorg. Med. Chem. 16, 7270-6, (2008)
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The contribution of plukenetione A to the anti-tumoral activity of Cuban propolis. David Díaz-Carballo et al Bioorg. Med. Chem. 16, 9635-43, (2008)
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Synthesis and molecular modelling of unsaturated exomethylene pyranonucleoside analogues with antitumor and antiviral activities. George Agelis et al Eur. J. Med. Chem. 43, 1366-75, (2008)
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Regiospecific microwave-assisted synthesis and cytotoxic activity against human breast cancer cells of (RS)-6-substituted-7- or 9-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-7H- or -9H-purines. Ana Conejo-García et al Eur. J. Med. Chem. 43, 1742-8, (2008)
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Unsaturated fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-4-keto-beta-d-glucopyranosyl derivatives of N(4)-benzoyl cytosine and N(6)-benzoyl adenine. Stella Manta et al Eur. J. Med. Chem. 43, 420-8, (2008)
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Diterpenoids from the roots of Suregada glomerulata. Ren-Yi Yan et al J. Nat. Prod. 71, 195-8, (2008)
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Cytotoxic hydrolyzable tannins from Balanophora japonica. Zhi-Hong Jiang et al J. Nat. Prod. 71, 719-23, (2008)
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Kadsuracoccinic acids A-C, ring-A seco-lanostane triterpenes from Kadsura coccinea and their effects on embryonic cell division of Xenopus laevis. Heran Li et al J. Nat. Prod. 71, 739-41, (2008)
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Lanostane-type triterpenoids from the roots of Kadsura coccinea. Nan Wang et al J. Nat. Prod. 71, 990-4, (2008)
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A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Montagnoli, A., et al. Nat. Chem. Biol. 4, 357-365, (2008)
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Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. R Scott Obach et al Drug Metab. Dispos. 36, 1385-405, (2008)
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Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. Naomi L Kruhlak et al Toxic. Mech. Methods 18, 217-27, (2008)
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High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors. Younis Baqi et al J. Med. Chem. 52, 3784-93, (2009)
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Physicochemical determinants of human renal clearance. Manthena V S Varma et al J. Med. Chem. 52, 4844-52, (2009)
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Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies. Aurélien Putey et al J. Med. Chem. 52, 5916-25, (2009)
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Microwave-assisted synthesis of N-substituted cyclic imides and their evaluation for anticancer and anti-inflammatory activities. Sham M Sondhi et al Bioorg. Med. Chem. Lett. 19, 1534-8, (2009)
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Porphyrins containing nitric oxide donors: Synthesis and cancer cell-oriented NO release. Wukun Liu et al Bioorg. Med. Chem. Lett. 19, 1647-9, (2009)
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Synthesis of potent antitumor and antiviral benzofuran derivatives. Shadia A Galal et al Bioorg. Med. Chem. Lett. 19, 2420-8, (2009)
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Design, synthesis and anticancer activities of hybrids of indole and barbituric acids--identification of highly promising leads. Palwinder Singh et al Bioorg. Med. Chem. Lett. 19, 3054-8, (2009)
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In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives. Julia K J Ahlskog et al Bioorg. Med. Chem. Lett. 19, 4851-6, (2009)
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Sesquiterpenoids from Pilea cavaleriei subsp. crenata. Gui-Hua Tang et al Bioorg. Med. Chem. Lett. 19, 5737-40, (2009)
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A facile synthesis and biological activity of novel tetrahydrobenzo[4',5']thieno[3',2':5,6]pyrido[4,3-d]pyrimidin-4(3H)-ones. Qingyun Ren et al Bioorg. Med. Chem. Lett. 19, 6713-6, (2009)
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Synthesis and biological evaluation of novel conjugates of podophyllotoxin and 5-FU as antineoplastic agents. Shi-Wu Chen et al Bioorg. Med. Chem. 17, 3111-7, (2009)
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Preparation of novel (Z)-4-ylidenebenzo[b]furo[3,2-d][1,3]oxazines and their biological activity. Yukako Tabuchi et al Bioorg. Med. Chem. 17, 3959-67, (2009)
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Synthesis, antitumor evaluation, molecular modeling and quantitative structure-activity relationship (QSAR) of some novel arylazopyrazolodiazine and triazine analogs. Ahmed El-Shafei et al Bioorg. Med. Chem. 17, 5096-105, (2009)
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Tessaric acid derivatives induce G2/M cell cycle arrest in human solid tumor cell lines. Leticia G León et al Bioorg. Med. Chem. 17, 6251-6, (2009)
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Synthesis of modified pyrimidine bases and positive impact of chemically reactive substituents on their in vitro antiproliferative activity. Steffi Noll et al Eur. J. Med. Chem. 44, 1172-9, (2009)
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Substituted quinazolines, part 3. Synthesis, in vitro antitumor activity and molecular modeling study of certain 2-thieno-4(3H)-quinazolinone analogs. Abdulrahman M Al-Obaid et al Eur. J. Med. Chem. 44, 2379-91, (2009)
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Novel 2,4,5-trisubstituted oxazole derivatives: synthesis and antiproliferative activity. Xin-Hua Liu et al Eur. J. Med. Chem. 44, 3930-5, (2009)
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Novel modified steroid derivatives of androstanolone as chemotherapeutic anti-cancer agents. Mohamed El-Far et al Eur. J. Med. Chem. 44, 3936-46, (2009)
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Synthesis of substituted-phenyl-1,2,4-triazol-3-thione analogues with modified D-glucopyranosyl residues and their antiproliferative activities. Zhizhang Li et al Eur. J. Med. Chem. 44, 4716-20, (2009)
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Synthesis and anticancer activity of N-bis(trifluoromethyl)alkyl-N'-thiazolyl and N-bis(trifluoromethyl)alkyl-N'-benzothiazolyl ureas. Elena L Luzina et al Eur. J. Med. Chem. 44, 4944-53, (2009)
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A Ser29Leu substitution in the cytosine deaminase Fca1p is responsible for clade-specific flucytosine resistance in Candida dubliniensis. Brenda A McManus et al Antimicrob. Agents Chemother. 53, 4678-85, (2009)
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Pyrrolidinoindoline alkaloids from Selaginella moellendorfii. Yue-Hu Wang et al J. Nat. Prod. 72, 1151-4, (2009)
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Chemical constituents of propolis from Myanmar and their preferential cytotoxicity against a human pancreatic cancer cell line. Feng Li et al J. Nat. Prod. 72, 1283-7, (2009)
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Cycloaspeptides F and G, Cyclic Pentapeptides from a Cordyceps-colonizing isolate of Isaria farinosa. Yonggang Zhang et al J. Nat. Prod. 72, 1364-7, (2009)
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Isoprenylated chromone derivatives from the plant endophytic fungus Pestalotiopsis fici. Ling Liu et al J. Nat. Prod. 72, 1482-6, (2009)
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Cytotoxic constituents of Soymida febrifuga from Myanmar. Suresh Awale et al J. Nat. Prod. 72, 1631-6, (2009)
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Allenyl and alkynyl phenyl ethers from the endolichenic fungus Neurospora terricola. Fan Zhang et al J. Nat. Prod. 72, 1782-5, (2009)
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Quassinoids from Eurycoma longifolia. Katsunori Miyake et al J. Nat. Prod. 72, 2135-40, (2009)
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Pyrrolidinones from the ascomycete fungus Albonectria rigidiuscula. Jian Li et al J. Nat. Prod. 72, 2184-7, (2009)
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2-Arylbenzofuran Derivatives from Morus cathayana. Gang Ni et al J. Nat. Prod. 72, 966-8, (2009)
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Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. Jing Yuan et al Nat. Chem. Biol. 5, 765-71, (2009)
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Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. Ashley Jarvis et al J. Med. Chem. 53, 2215-26, (2010)
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A series of alpha-heterocyclic carboxaldehyde thiosemicarbazones inhibit topoisomerase IIalpha catalytic activity. He Huang et al J. Med. Chem. 53, 3048-64, (2010)
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Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. Menichincheri, M.; et al. J. Med. Chem. 53, 7296, (2010)
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Synthesis, chiral resolution, and determination of novel furan lignan derivatives with potent anti-tumor activity. Hai Ling Sun et al Bioorg. Med. Chem. Lett. 20, 1961-4, (2010)
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Bio-transformation of artemisinin using soil microbe: Direct C-acetoxylation of artemisinin at C-9 by Penicillium simplissimum. Abhishek Goswami et al Bioorg. Med. Chem. Lett. 20, 359-61, (2010)
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Synthesis and molecular docking studies of novel 2-chloro-pyridine derivatives containing flavone moieties as potential antitumor agents X. Liu, et al., Bioorg. Med. Chem. Lett. 20, 4163-4167, (2010)
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Synthesis and molecular docking study of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential antitumor agents. Xin-Hua Liu et al Bioorg. Med. Chem. Lett. 20, 5705-8, (2010)
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Synthesis, X-ray crystal structure study and antitumoral evaluations of 5,6-disubstituted pyrimidine derivatives. Tatjana Gazivoda Kraljevi? et al Bioorg. Med. Chem. 18, 2704-12, (2010)
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Non-classical antifolates. Part 2: synthesis, biological evaluation, and molecular modeling study of some new 2,6-substituted-quinazolin-4-ones. Fatmah A M Al-Omary et al Bioorg. Med. Chem. 18, 2849-63, (2010)
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Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines. José C Aponte et al Bioorg. Med. Chem. 18, 2880-6, (2010)
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Aplysinopsin analogs: synthesis and anti-proliferative activity of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones Thirupathi R. Y.; et al. Bioorg. Med. Chem. 18, 3570, (2010)
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Novel nucleosides as potent influenza viral inhibitors. Manohar Sharma Vedula et al Bioorg. Med. Chem. 18, 6329-39, (2010)
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Effect of goniothalamin on the development of Ehrlich solid tumor in mice. Débora Barbosa Vendramini-Costa et al Bioorg. Med. Chem. 18, 6742-7, (2010)
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QSAR-based solubility model for drug-like compounds. Rafael Gozalbes et al Bioorg. Med. Chem. 18, 7078-84, (2010)
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Synthesis, biological evaluation, and molecular docking studies of 2-chloropyridine derivatives possessing 1,3,4-oxadiazole moiety as potential antitumor agents. Qing-Zhong Zheng et al Bioorg. Med. Chem. 18, 7836-41, (2010)
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Synthesis and anticancer activity of new 1-[(5 or 6-substituted 2-alkoxyquinoxalin-3-yl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives. Young Bok Lee et al Bioorg. Med. Chem. 18, 7966-74, (2010)
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Synthesis of 4?-N-polyaromatic substituted podophyllotoxins: DNA topoisomerase inhibition, anticancer and apoptosis-inducing activities. Ahmed Kamal et al Bioorg. Med. Chem. 18, 8493-500, (2010)
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Developing structure-activity relationships for the prediction of hepatotoxicity. Nigel Greene et al Chem. Res. Toxicol. 23, 1215-22, (2010)
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Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. Denis Fourches et al Chem. Res. Toxicol. 23, 171-83, (2010)
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Synthesis of new pyrrolo[2,3-d]pyrimidine derivatives and evaluation of their activities against human colon cancer cell lines. Saritha Jyostna Tangeda et al Eur. J. Med. Chem. 45, 1453-8, (2010)
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QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations. Andrey A Toropov et al Eur. J. Med. Chem. 45, 1639-47, (2010)
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Novel benzimidazole-pyrimidine conjugates as potent antitumor agents. Heba T Abdel-Mohsen et al Eur. J. Med. Chem. 45, 2336-44, (2010)
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Synthesis, anticancer and antioxidant activities of 7-methoxyisoflavanone and 2,3-diarylchromanones. Kanagasabai Kanagalakshmi et al Eur. J. Med. Chem. 45, 2447-52, (2010)
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Novel effects of glycyrrhetinic acid on the central nervous system tumorigenic progenitor cells: induction of actin disruption and tumor cell-selective toxicity. Hideaki Yamaguchi et al Eur. J. Med. Chem. 45, 2943-8, (2010)
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Synthesis and antitumor activity of novel 2',3'-diethanethio-2',3',5'-trideoxy-5'-triazolonucleoside analogues. Jin-Lan Yu et al Eur. J. Med. Chem. 45, 3219-22, (2010)
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Synthesis and antitumor activity of liquiritigenin thiosemicarbazone derivatives. Kun Hu et al Eur. J. Med. Chem. 45, 3453-8, (2010)
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Synthesis and cytotoxic activity of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidine derivatives. Miguel Angel Vilchis-Reyes et al Eur. J. Med. Chem. 45, 379-86, (2010)
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Anticancer activity of N-bis(trifluoromethyl)alkyl-N'-(polychlorophenyl) and N'-(1,2,4-triazolyl) ureas. Elena L Luzina et al Eur. J. Med. Chem. 45, 5507-12, (2010)
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Synthesis, anti-inflammatory and anticancer activity evaluation of some novel acridine derivatives. Sham M Sondhi et al Eur. J. Med. Chem. 45, 555-63, (2010)
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Synthesis, antitumor activity and molecular docking study of novel sulfonamide-Schiff's bases, thiazolidinones, benzothiazinones and their C-nucleoside derivatives. Mohsen M Kamel et al Eur. J. Med. Chem. 45, 572-80, (2010)
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Semi-synthesis and anti-tumor activity of 5,8-O-dimethyl acylshikonin derivatives. Wen Zhou et al Eur. J. Med. Chem. 45, 6005-11, (2010)
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Cytotoxic activity of 3-(5-phenyl-3H-[1,2,4]dithiazol-3-yl)chromen-4-ones and 4-oxo-4H-chromene-3-carbothioic acid N-phenylamides. Tilak Raj et al Eur. J. Med. Chem. 45, 790-4, (2010)
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Triterpenoids and steroids from the fruits of Melia toosendan and their cytotoxic effects on two human cancer cell lines. Shi-Biao Wu et al J. Nat. Prod. 73, 1898-906, (2010)
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Oxepinochromenones, furochromenone, and their putative precursors from the endolichenic fungus Coniochaeta sp. Yinchao Wang et al J. Nat. Prod. 73, 920-4, (2010)
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Antiproliferative activity of withanolides against human breast cancer cell lines. Rubén P Machin et al J. Nat. Prod. 73, 966-8, (2010)
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A predictive ligand-based Bayesian model for human drug-induced liver injury. Sean Ekins et al Drug Metab. Dispos. 38, 2302-8, (2010)
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3,5-Bis(benzylidene)-1-[3-(2-hydroxyethylthio)propanoyl]piperidin-4-ones: a novel cluster of potent tumor-selective cytotoxins. Umashankar Das et al J. Med. Chem. 54, 3445-9, (2011)
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N-fused imidazoles as novel anticancer agents that inhibit catalytic activity of topoisomerase II? and induce apoptosis in G1/S phase. Ashish T Baviskar et al J. Med. Chem. 54, 5013-30, (2011)
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Efficient synthesis and biological evaluation of 1,3-benzenedicarbonyl dithioureas. Hao Peng et al Bioorg. Med. Chem. Lett. 21, 1102-4, (2011)
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Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents. Xin-Hua Liu et al Bioorg. Med. Chem. Lett. 21, 2916-20, (2011)
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Synthesis and in vitro cytotoxic evaluation of N-alkylbromo and N-alkylphthalimido-isatins. Pardeep Singh et al Bioorg. Med. Chem. Lett. 21, 3017-20, (2011)
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Synthesis and in vitro antitumor activity of new butenolide-containing dithiocarbamates. Xiao-Juan Wang et al Bioorg. Med. Chem. Lett. 21, 3074-7, (2011)
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Synthesis and anti-tumor activity of novel ethyl 3-aryl-4-oxo-3,3a,4,6-tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylates. Tiantian Wang et al Bioorg. Med. Chem. Lett. 21, 3381-3, (2011)
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Antiproliferative and apoptotic sesquiterpene lactones from Carpesium faberi. Xu-Wen Li et al Bioorg. Med. Chem. Lett. 21, 366-72, (2011)
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Synthesis and cytotoxicity of 8-cyano-3-substitutedalkyl-5-methyl-4-methylene-7-methoxy-3,4-dihydropyrido[4,3-d]pyrimidines. Wen-Yan Mo et al Bioorg. Med. Chem. Lett. 21, 5975-7, (2011)
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Synthesis, biological evaluation and molecular docking studies of 1,3,4-thiadiazole derivatives containing 1,4-benzodioxan as potential antitumor agents. Juan Sun et al Bioorg. Med. Chem. Lett. 21, 6116-21, (2011)
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Synthesis of 4β-carbamoyl epipodophyllotoxins as potential antitumour agents. Kamal, A.; et al. Bioorg. Med. Chem. 19, 2975, (2011)
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Selective bone targeting 5-fluorouracil prodrugs: synthesis and preliminary biological evaluation. Liang Ouyang et al Bioorg. Med. Chem. 19, 3750-6, (2011)
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New class azaphilone produced by a marine fish-derived Chaetomium globosum. The stereochemistry and biological activities. Takeshi Yamada et al Bioorg. Med. Chem. 19, 4106-13, (2011)
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Antifungal thiopeptide cyclothiazomycin B1 exhibits growth inhibition accompanying morphological changes via binding to fungal cell wall chitin. Naoko Mizuhara et al Bioorg. Med. Chem. 19, 5300-10, (2011)
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Synthesis and antitumor activity of ?-carboline 3-(substituted-carbohydrazide) derivatives. Valéria Aquilino Barbosa et al Bioorg. Med. Chem. 19, 6400-8, (2011)
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Synthesis, biological evaluation, and molecular docking studies of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan moiety as potential anticancer agents. Xiao-Min Zhang et al Bioorg. Med. Chem. 19, 6518-24, (2011)
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2-Anilinonicotinyl linked 2-aminobenzothiazoles and [1,2,4]triazolo[1,5-b] [1,2,4]benzothiadiazine conjugates as potential mitochondrial apoptotic inducers. Ahmed Kamal et al Bioorg. Med. Chem. 19, 7136-50, (2011)
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Synthesis, antimicrobial, antioxidant, anti-hemolytic and cytotoxic evaluation of new imidazole-based heterocycles. Bakr F Abdel-Wahab et al Eur. J. Med. Chem. 46, 1505-11, (2011)
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Cytotoxic and protective DNA damage of three new diterpenoids from the brown alga Dictoyota dichotoma. Seif-Eldin N Ayyad et al Eur. J. Med. Chem. 46, 175-82, (2011)
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Synthesis and biological evaluation of novel 2-aralkyl-5-substituted-6-(4'-fluorophenyl)-imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent anticancer agents. Subhas S Karki et al Eur. J. Med. Chem. 46, 2109-16, (2011)
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Synthesis and in vitro anti-tumor activity of new oxadiazole thioglycosides. M A Abu-Zaied et al Eur. J. Med. Chem. 46, 229-35, (2011)
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New (RS)-benzoxazepin-purines with antitumour activity: The chiral switch from (RS)-2,6-dichloro-9-[1-(p-nitrobenzenesulfonyl)-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl]-9H-purine. Luisa C López-Cara et al Eur. J. Med. Chem. 46, 249-58, (2011)
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Novel imidazo[4,5-b]pyridine and triaza-benzo[c]fluorene derivatives: synthesis, antiproliferative activity and DNA binding studies. Marijana Hranjec et al Eur. J. Med. Chem. 46, 2748-58, (2011)
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Design, synthesis and in vitro drug release investigation of new potential 5-FU prodrugs. Pierre Daumar et al Eur. J. Med. Chem. 46, 2867-79, (2011)
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Synthesis, antitumor and antimicrobial activities of 4-(4-chlorophenyl)-3-cyano-2-(?-O-glycosyloxy)-6-(thien-2-yl)-nicotinonitrile. Hassan A El-Sayed et al Eur. J. Med. Chem. 46, 2948-54, (2011)
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Anti-proliferative activity of aguerin B and a new rare nor-guaianolide lactone isolated from the aerial parts of Centaurea deflexa. Andrea Chicca et al Eur. J. Med. Chem. 46, 3066-70, (2011)
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Design and synthesis of spiro derivatives of parthenin as novel anti-cancer agents. Doma Mahendhar Reddy et al Eur. J. Med. Chem. 46, 3210-7, (2011)
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Semi-synthesis and antitumor activity of 6-isomers of 5, 8-O-dimethyl acylshikonin derivatives. Wen Zhou et al Eur. J. Med. Chem. 46, 3420-7, (2011)
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Synthesis and antitumor activity of new sulfonamide derivatives of thiadiazolo[3,2-a]pyrimidines. Nadia S El-Sayed et al Eur. J. Med. Chem. 46, 3714-20, (2011)
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Anticancer activity and cDNA microarray studies of a (RS)-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl]-6-chloro-9H-purine, and an acyclic (RS)-O,N-acetalic 6-chloro-7H-purine. Octavio Caba et al Eur. J. Med. Chem. 46, 3802-9, (2011)
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Synthesis, biological evaluation of chrysin derivatives as potential immunosuppressive agents. Peng-Cheng Lv et al Eur. J. Med. Chem. 46, 393-8, (2011)
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Synthesis and antitumour activity of ?-hydroxyisovalerylshikonin analogues. Zhen Rao et al Eur. J. Med. Chem. 46, 3934-41, (2011)
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Synthesis and antitumor activity of ureas containing pyrimidinyl group. Chuanfei Jin et al Eur. J. Med. Chem. 46, 429-32, (2011)
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Branched-chain C-cyano pyranonucleosides: synthesis of 3'-C-cyano & 3'-C-cyano-3'-deoxy pyrimidine pyranonucleosides as novel cytotoxic agents. Christos Kiritsis et al Eur. J. Med. Chem. 46, 5668-74, (2011)
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Synthesis and cytotoxic activity of novel 3-(1H-indol-3-yl)-1H-pyrazole-5-carbohydrazide derivatives. Datong Zhang et al Eur. J. Med. Chem. 46, 5868-77, (2011)
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Synthesis of new C5-(1-substituted-1,2,3-triazol-4 or 5-yl)-2'-deoxyuridines and their antiviral evaluation. Aurélien Montagu et al Eur. J. Med. Chem. 46, 778-86, (2011)
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Investigations on cytotoxicity and anti-inflammatory potency of licofelone derivatives. Wukun Liu et al Eur. J. Med. Chem. 46, 907-13, (2011)
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Synthesis and biological evaluation of unsaturated keto and exomethylene D-arabinopyranonucleoside analogs: novel 5-fluorouracil analogs that target thymidylate synthase. Niki Tzioumaki et al Eur. J. Med. Chem. 46, 993-1005, (2011)
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Triazole and dihydroimidazole alkaloids from the marine sediment-derived fungus Penicillium paneum SD-44. Chun-Shun Li et al J. Nat. Prod. 74, 1331-4, (2011)
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Cytotoxic and apoptosis-inducing activities of triterpene acids from Poria cocos. Takashi Kikuchi et al J. Nat. Prod. 74, 137-44, (2011)
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Nigerapyrones A-H, ?-pyrone derivatives from the marine mangrove-derived endophytic fungus Aspergillus niger MA-132. Dong Liu et al J. Nat. Prod. 74, 1787-91, (2011)
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Cytotoxic bistetrahydrofuran annonaceous acetogenins from the seeds of Annona squamosa. Yong Chen et al J. Nat. Prod. 74, 2477-81, (2011)
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Comazaphilones A-F, azaphilone derivatives from the marine sediment-derived fungus Penicillium commune QSD-17. Shu-Shan Gao et al J. Nat. Prod. 74, 256-61, (2011)
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Cytotoxic and apoptosis-inducing activities of limonoids from the seeds of Azadirachta indica (neem). Takashi Kikuchi et al J. Nat. Prod. 74, 866-70, (2011)
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Translating Clinical Findings into Knowledge in Drug Safety Evaluation - Drug Induced Liver Injury Prediction System (DILIps). Zhichao Liu et al PLoS Comput. Biol. 7, e1002310, (2011)
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Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives. Tatjana Gazivoda Kraljevi? et al Bioorg. Med. Chem. Lett. 22, 308-12, (2012)
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Acyl derivatives of boswellic acids as inhibitors of NF-?B and STATs. Ajay Kumar et al Bioorg. Med. Chem. Lett. 22, 431-5, (2012)
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Synthesis and in vitro antiproliferative evaluation of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives. Yong Ai et al Eur. J. Med. Chem. 47, 206-13, (2012)
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Synthesis and antitumor activity of conjugates of 5-Fluorouracil and emodin. Li-Ming Zhao et al Eur. J. Med. Chem. 47, 255-60, (2012)
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Novel 1,3,4-heterodiazole analogues: synthesis and in-vitro antitumor activity. Azza T Taher et al Eur. J. Med. Chem. 47, 445-51, (2012)
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1,2,3-Triazole tethered ?-lactam-Chalcone bifunctional hybrids: synthesis and anticancer evaluation. Pardeep Singh et al Eur. J. Med. Chem. 47, 594-600, (2012)
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Substituted thiazoles V. synthesis and antitumor activity of novel thiazolo[2,3-b]quinazoline and pyrido[4,3-d]thiazolo[3,2-a]pyrimidine analogues. Fatmah A M Al-Omary et al Eur. J. Med. Chem. 47, 65-72, (2012)
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Synthesis, antimicrobial, anticancer evaluation and QSAR studies of 6-methyl-4-[1-(2-substituted-phenylamino-acetyl)-1H-indol-3-yl]-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl esters. Sandeep Kumar Sharma et al Eur. J. Med. Chem. 48, 16-25, (2012)
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Synthesis and antitumor evaluation of some new 1,3,4-oxadiazole-based heterocycles. Samir Bondock et al Eur. J. Med. Chem. 48, 192-9, (2012)
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Synthesis and cytotoxicity of O,O'-dialkyl {[2-(substituted phenoxy)acetamido](substituted phenyl)methyl}phosphonates. Lihong Ning et al Eur. J. Med. Chem. 48, 379-84, (2012)
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Synthesis of novel 2, 5-dihydrofuran derivatives and evaluation of their anticancer activity. Yikai Zhang et al Eur. J. Med. Chem. 48, 69-80, (2012)
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Synthesis and evaluation of anticancer activity of some novel 6-aryl-2-(p-sulfamylphenyl)-pyridazin-3(2H)-ones. I G Rathish et al Eur. J. Med. Chem. 49C, 304-9, (2012)
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Synthesis and biological evaluation of conjugates of deoxypodophyllotoxin and 5-FU as inducer of caspase-3 and -7. Wen-Ting Huang et al Eur. J. Med. Chem. 49C, 48-54, (2012)
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Bakuchiol derivatives as novel and potent cytotoxic agents: A report. Rabiya Majeed et al Eur. J. Med. Chem. 49C, 55-67, (2012)
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Structure-activity studies on the anti-proliferation activity of ajoene analogues in WHCO1 oesophageal cancer cells. Catherine H Kaschula et al Eur. J. Med. Chem. 50, 236-54, (2012)
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Merck 14,4181
Beil. 24,IV,1229
Aldrich MSDS 1, 978:A / Corp MSDS 1 (1), 1731:B / FT-IR 1 (2), 809:D / FT-IR 2 (3), 3829:C / FT-NMR 1 (3), 362:C / IR-Spectra (3), 1353:H / IR-Spectra (2), 1179:B / NMR-Reference 2 (2), 690:D / RegBook 1 (2), 2565:C / Sax 6, 1449 / Sigma FT-IR 1 (1), 996:C / Structure Index 1, 405:D:4