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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
Traditional Medicinals and Cancer
Traditional Chinese Medicine (TCM) is a healing art that has been practiced for thousands of years. The practice of TCM is a holistic approach that includes the use of herbal preparations, acupunctur...
Lynn Stephenson, Product Specialist, Sigma® Life Science and Chloe McClanahan, Product Manager, Sigma Life Science
Biofiles Vol. 8, No. 6
Keywords: Analgesics, Antitumor agents, Apoptosis, Cancer, Drug discovery, Fractionation, High performance liquid chromatography, Metabolites, Metabolomics, Nuclear magnetic resonance spectroscopy, Pharmaceutical
Papers
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Molecular modeling studies of the DNA-topoisomerase I ternary cleavable complex with camptothecin. Fan, Y., et al. J. Med. Chem. 41, 2216-2226, (1998)
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Mechanism of action of eukaryotic DNA topoisomerase I and drugs targeted to the enzyme. Pommier, Y., et al. Biochim. Biophys. Acta 1400, 83-105, (1998)
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Ubiquitin-dependent destruction of topoisomerase I is stimulated by the antitumor drug camptothecin. Desai, S. D., et al. J. Biol. Chem. 272, 24159-24164, (1997)
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Camptothecin induction of a time- and concentration-dependent decrease of topoisomerase I and its implication in camptothecin activity. Beidler, D.R., and Cheng, Y.C. Mol. Pharmacol. 47, 907-914, (1994)
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Replication-dependent and -independent camptothecin cytotoxicity of seven human colon tumor cell lines. Borovitskaya, A.E., and D-Arpa, P. Oncol. Res. 10, 271-276, (1998)
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Induction of neuronal apoptosis by camptothecin, an inhibitor of DNA topoisomerase-I: evidence for cell cycle-independent toxicity. Morris. E.J., and Geller, H.M. J. Cell Biol. 134, 757-770, (1996)
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Cell death induced by topoisomerase-targeted drugs: more questions than answers. Kaufmann, S. H. Biochim. Biophys. Acta 1400, 195-211, (1998)
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Pseudomonas Aeruginosa Eliminates Natural Killer Cells Via Phagocytosis-induced Apoptosis. Chung, J.W., et al. PLoS Pathog. 5, e1000561, (2009)
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High Levels Of Hsp90 Cochaperone P23 Promote Tumor Progression And Poor Prognosis In Breast Cancer By Increasing Lymph Node Metastases And Drug Resistance. Simpson, N.E., et al. Cancer Res. 70, 8446-56, (2010)
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Neurotoxic Activity Of A Topoisomerase-I Inhibitor, Camptothecin, In Cultured Cerebellar Granule Neurons. Uday Bhanu, M., and Kondapi, A.K. Neurotoxicology 31, 730-7, (2010)
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Inversin Relays Frizzled-8 Signals To Promote Proximal Pronephros Development. Lienkamp, S., et al. Proc. Natl. Acad. Sci. U. S. A. 107, 20388-93, (2010)
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Induction of apoptosis in human cancer cells by candidaspongiolide, a novel sponge polyketide. Daniela Trisciuoglio et al J. Natl. Cancer Inst. 100, 1233-46, (2008)
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Synthesis, antitumor evaluation, and apoptosis-inducing activity of hydroxylated (E)-stilbenes. Cedric J Lion et al J. Med. Chem. 48, 1292-5, (2005)
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CHMIS-C: a comprehensive herbal medicine information system for cancer. Xueliang Fang et al J. Med. Chem. 48, 1481-8, (2005)
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Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex. Bart L Staker et al J. Med. Chem. 48, 2336-45, (2005)
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1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities. Gary T Wang et al J. Med. Chem. 48, 3118-21, (2005)
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Molecular determinants of topoisomerase I poisoning by lamellarins: comparison with camptothecin and structure-activity relationships. Esther Marco et al J. Med. Chem. 48, 3796-807, (2005)
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Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis. Alexandra Ioanoviciu et al J. Med. Chem. 48, 4803-14, (2005)
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Camptothecin binds to a synthetic peptide identified by a T7 phage display screen. Yoichi Takakusagi et al Bioorg. Med. Chem. Lett. 15, 4850-3, (2005)
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DNA topoisomerase I inhibitors from Rinorea anguifera. Ji Ma et al Bioorg. Med. Chem. Lett. 15, 813-6, (2005)
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New colchicinoids from a native Jordanian meadow saffron, colchicum brachyphyllum: isolation of the first naturally occurring dextrorotatory colchicinoid. Feras Q Alali et al J. Nat. Prod. 68, 173-8, (2005)
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Indole alkaloids and other constituents of Rauwolfia serpentina. Atsuko Itoh et al J. Nat. Prod. 68, 848-52, (2005)
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Synthesis and antitumor characterization of pyrazolic analogues of the marine pyrroloquinoline alkaloids: wakayin and tsitsikammamines. Laurent Legentil et al J. Med. Chem. 49, 2979-88, (2006)
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Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors. Muthukaman Nagarajan et al J. Med. Chem. 49, 5129-40, (2006)
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Nuphar alkaloids with immediately apoptosis-inducing activity from Nuphar pumilum and their structural requirements for the activity. Hisashi Matsuda et al Bioorg. Med. Chem. Lett. 16, 1567-73, (2006)
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Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors. Andrew Morrell et al Bioorg. Med. Chem. Lett. 16, 1846-9, (2006)
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Design and semisynthesis of novel fredericamycin A derivatives with an improved antitumor profile. Ulrich Abel et al Bioorg. Med. Chem. Lett. 16, 3292-7, (2006)
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Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay. Andrew Morrell et al Bioorg. Med. Chem. Lett. 16, 4395-9, (2006)
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Microwave expedited synthesis of 5-aminocamptothecin analogs: Inhibitors of hypoxia inducible factor HIF-1alpha. Joelle Torregrossa et al Bioorg. Med. Chem. Lett. 16, 6082-5, (2006)
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Cytotoxic and other compounds from Didymochlaena truncatula from the Madagascar rain forest. Shugeng Cao et al J. Nat. Prod. 69, 284-6, (2006)
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Identifying off-target effects and hidden phenotypes of drugs in human cells. Marnie L MacDonald et al Nat. Chem. Biol. 2, 329-37, (2006)
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Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures. Andrew Morrell et al J. Med. Chem. 50, 2040-8, (2007)
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Synthesis, DNA binding, and Leishmania topoisomerase inhibition activities of a novel series of anthra[1,2-d]imidazole-6,11-dione derivatives. Padmaparna Chaudhuri et al J. Med. Chem. 50, 2536-40, (2007)
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Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors. Le Wang et al J. Med. Chem. 50, 4162-76, (2007)
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Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors. Andrew Morrell et al J. Med. Chem. 50, 4388-404, (2007)
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Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization. Andrew Morrell et al J. Med. Chem. 50, 4419-30, (2007)
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Antitumor agents. 256. Conjugation of paclitaxel with other antitumor agents: evaluation of novel conjugates as cytotoxic agents. Kyoko Nakagawa-Goto et al Bioorg. Med. Chem. Lett. 17, 2894-8, (2007)
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Design, docking, and synthesis of novel indeno[1,2-c]isoquinolines for the development of antitumor agents as topoisomerase I inhibitors. Won-Jea Cho et al Bioorg. Med. Chem. Lett. 17, 3531-4, (2007)
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Convenient synthesis of indeno[1,2-c]isoquinolines as constrained forms of 3-arylisoquinolines and docking study of a topoisomerase I inhibitor into DNA-topoisomerase I complex. Hue Thi My Van et al Bioorg. Med. Chem. Lett. 17, 5763-7, (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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Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa. Hisashi Matsuda et al Bioorg. Med. Chem. 15, 1539-46, (2007)
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Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones. Hee-Kyung Rhee et al Bioorg. Med. Chem. 15, 1651-8, (2007)
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Biological profile of new apoptotic agents based on 2,4-pyrido[2,3-d]pyrimidine derivatives. Lucía Cordeu et al Bioorg. Med. Chem. 15, 1659-69, (2007)
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Naphthoindole-based analogues of tryptophan and tryptamine: synthesis and cytotoxic properties. Andrey E Shchekotikhin et al Bioorg. Med. Chem. 15, 2651-9, (2007)
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Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Yunsong Tong et al Bioorg. Med. Chem. 15, 2759-67, (2007)
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Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted luotonin A derivatives. Kassoum Nacro et al Bioorg. Med. Chem. 15, 4237-46, (2007)
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Synthesis of 6-chloroisoquinoline-5,8-diones and pyrido[3,4-b]phenazine-5,12-diones and evaluation of their cytotoxicity and DNA topoisomerase II inhibitory activity. Jin Sung Kim et al Bioorg. Med. Chem. 15, 451-7, (2007)
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Inhibition of colon cancer cell growth and antioxidant activity of bioactive compounds from Poncirus trifoliata (L.) Raf. G K Jayaprakasha et al Bioorg. Med. Chem. 15, 4923-32, (2007)
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Synthesis of ferulic ester dimers, functionalisation and biological evaluation as potential antiatherogenic and antiplasmodial agents. D L A Rakotondramanana et al Bioorg. Med. Chem. 15, 6018-26, (2007)
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Synthesis and antiproliferative properties of N3/8-disubstituted 3,8-diazabicyclo[3.2.1]octane analogues of 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl-piperazine. Rosanna Filosa et al Eur. J. Med. Chem. 42, 293-306, (2007)
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Curcumin induces high levels of topoisomerase I- and II-DNA complexes in K562 leukemia cells. Miguel López-Lázaro et al J. Nat. Prod. 70, 1884-8, (2007)
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Cells lacking DNA topoisomerase II beta are resistant to genistein. Miguel López-Lazaro et al J. Nat. Prod. 70, 763-7, (2007)
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Vasorelaxant activity of diterpenes from Croton zambesicus and synthetic trachylobanes and their structure-activity relationships. Chiara Baccelli et al J. Nat. Prod. 70, 910-7, (2007)
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Alvaradoins E-N, antitumor and cytotoxic anthracenone C-glycosides from the leaves of Alvaradoa haitiensis. Sharnelle S Phifer et al J. Nat. Prod. 70, 954-61, (2007)
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Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Mai Nguyen et al Proc. Natl. Acad. Sci. U. S. A. 104, 19512-7, (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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Thiocamptothecin. Cristian Samorì et al J. Med. Chem. 51, 3040-4, (2008)
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Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors. Maris A Cinelli et al J. Med. Chem. 51, 4609-19, (2008)
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Novel amidino-substituted thienyl- and furylvinylbenzimidazole: derivatives and their photochemical conversion into corresponding diazacyclopenta[c]fluorenes. synthesis, interactions with DNA and RNA, and antitumor evaluation. 4. Marijana Hranjec et al J. Med. Chem. 51, 4899-910, (2008)
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New insight for fluoroquinophenoxazine derivatives as possibly new potent topoisomerase I inhibitor. Da-Hye Kang et al Bioorg. Med. Chem. Lett. 18, 1520-4, (2008)
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E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation. Giuseppe Giannini et al Bioorg. Med. Chem. Lett. 18, 2910-5, (2008)
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Facile formation of hydrophilic derivatives of 5H-8,9-dimethoxy-5-[2-(N,N-dimethylamino)ethyl]-2,3-methylenedioxydibenzo[c,h] [1,6]naphthyridin-6-one (ARC-111) and its 12-aza analog via quaternary ammonium intermediates. Wei Feng et al Bioorg. Med. Chem. Lett. 18, 3570-2, (2008)
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Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring. Sheng Wang et al Bioorg. Med. Chem. Lett. 18, 4095-7, (2008)
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Chemotherapeutic bone-targeted bisphosphonate prodrugs with hydrolytic mode of activation. Rotem Erez et al Bioorg. Med. Chem. Lett. 18, 816-20, (2008)
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Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates. Ling-Wei Hsin et al Bioorg. Med. Chem. 16, 1006-14, (2008)
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Synthesis and antiproliferative evaluation of certain indeno[1,2-c]quinoline derivatives. Chih-Hua Tseng et al Bioorg. Med. Chem. 16, 3153-62, (2008)
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Synthesis, cytotoxic activities and structure-activity relationships of topoisomerase I inhibitors: indolizinoquinoline-5,12-dione derivatives. Yu Cheng et al Bioorg. Med. Chem. 16, 4617-25, (2008)
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Syntheses and biological evaluation of topoisomerase I-targeting agents related to 11-[2-(N,N-dimethylamino)ethyl]-2,3-dimethoxy-8,9-methylenedioxy-11H-isoquino[4,3-c]cinnolin-12-one (ARC-31). Mavurapu Satyanarayana et al Bioorg. Med. Chem. 16, 7824-31, (2008)
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Synthesis and structure-activity relationship studies of theophylline analogs on population responses in the rat hippocampus in vitro. Kethireddy V V Ananthalakshmi et al Bioorg. Med. Chem. 16, 8142-50, (2008)
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11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents. Wei Feng et al Bioorg. Med. Chem. 16, 8598-606, (2008)
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Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents. Wei Feng et al Bioorg. Med. Chem. 16, 9295-301, (2008)
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First synthesis of novel spin-labeled derivatives of camptothecin as potential antineoplastic agents. Ying-Qian Liu et al Eur. J. Med. Chem. 43, 2610-4, (2008)
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Synthesis of 2,6-diaryl-substituted pyridines and their antitumor activities. Jong-Keun Son et al Eur. J. Med. Chem. 43, 675-82, (2008)
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Characterization of an ABCG-like transporter from the protozoan parasite Leishmania with a role in drug resistance and transbilayer lipid movement. Esther Castanys-Muñoz et al Antimicrob. Agents Chemother. 52, 3573-9, (2008)
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Frajunolides E-K, briarane diterpenes from Junceella fragilis. Chia-Ching Liaw et al J. Nat. Prod. 71, 1551-6, (2008)
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Lignans from the roots of Saururus chinensis. Chang-Seob Seo et al J. Nat. Prod. 71, 1771-4, (2008)
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Cytotoxic triterpenoid saponins acylated with monoterpenic acid from Pithecellobium lucidum. Shuang Gang Ma et al J. Nat. Prod. 71, 41-6, (2008)
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Tasumatrols U-Z, taxane diterpene esters from Taxus sumatrana. Ya-Ching Shen et al J. Nat. Prod. 71, 576-80, (2008)
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Semisynthesis, biological activity, and molecular modeling studies of C-ring-modified camptothecins. Cristian Samorì et al J. Med. Chem. 52, 1029-39, (2009)
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Novel derivatives of pyridylbenzo[b]thiophene-2-carboxamides and benzo[b]thieno[2,3-c]naphthyridin-2-ones: minor structural variations provoke major differences of antitumor action mechanisms. Katja Ester et al J. Med. Chem. 52, 2482-92, (2009)
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Synthetic analogue of rocaglaol displays a potent and selective cytotoxicity in cancer cells: involvement of apoptosis inducing factor and caspase-12. Frédéric Thuaud et al J. Med. Chem. 52, 5176-87, (2009)
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Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification. Qi-Dong You et al J. Med. Chem. 52, 5649-61, (2009)
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Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues. Sonia G Das et al J. Med. Chem. 52, 5937-49, (2009)
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Molecular design, synthesis and docking study of benz[b]oxepines and 12-oxobenzo[c]phenanthridinones as topoisomerase 1 inhibitors. Suh-Hee Lee et al Bioorg. Med. Chem. Lett. 19, 2444-7, (2009)
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Structural modification of 3-arylisoquinolines to isoindolo[2,1-b]isoquinolinones for the development of novel topoisomerase 1 inhibitors with molecular docking study. Hue Thi My Van et al Bioorg. Med. Chem. Lett. 19, 2551-4, (2009)
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7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation. Mingzong Li et al Bioorg. Med. Chem. Lett. 19, 4107-9, (2009)
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On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents. Marina Gálvez-Peralta et al Bioorg. Med. Chem. Lett. 19, 4459-62, (2009)
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Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors. Hee-Ju Cho et al Bioorg. Med. Chem. Lett. 19, 6766-9, (2009)
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Bioactivity-guided isolation of cytotoxic constituents of Brucea javanica collected in Vietnam. Li Pan et al Bioorg. Med. Chem. 17, 2219-24, (2009)
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12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents. Feng, W.; et al. Bioorg. Med. Chem. 17, 2877, (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 and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships. Maris A Cinelli et al Bioorg. Med. Chem. 17, 7145-55, (2009)
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Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors. Hee-Kyung Rhee et al Bioorg. Med. Chem. 17, 7537-41, (2009)
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Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones. Lisa Sharma et al Eur. J. Med. Chem. 44, 1471-6, (2009)
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Photochemical electrocyclisation of 3-vinylindoles to pyrido[2,3-a]-, pyrido[4,3-a]- and thieno[2,3-a]-carbazoles: design, synthesis, DNA binding and antitumor cell cytotoxicity. Thomas Lemster et al Eur. J. Med. Chem. 44, 3235-52, (2009)
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Novel topoisomerase I-targeting antitumor agents synthesized from the N,N,N-trimethylammonium derivative of ARC-111, 5H-2,3-dimethoxy-8,9-methylenedioxy-5-[(2-N,N,N-trimethylammonium)ethyl]dibenzo[c,h][1,6]naphthyridin-6-one iodide. Wei Feng et al Eur. J. Med. Chem. 44, 3433-8, (2009)
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Synthesis and antitumoral activity of novel thiazolobenzotriazole, thiazoloindolo[3,2-c]quinoline and quinolinoquinoline derivatives. Anne Beauchard et al Eur. J. Med. Chem. 44, 3858-65, (2009)
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Activity of indenoisoquinolines against African trypanosomes. Rahul P Bakshi et al Antimicrob. Agents Chemother. 53, 123-8, (2009)
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Chemical constituents of Heteroplexis micocephala. Xiaona Fan et al J. Nat. Prod. 72, 1184-90, (2009)
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Cytotoxic triterpenoids from the rhizomes of Astilbe chinensis. Xing-Fu Cai et al J. Nat. Prod. 72, 1241-4, (2009)
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Candenatenins A-F, phenolic compounds from the heartwood of Dalbergia candenatensis. Sarot Cheenpracha et al J. Nat. Prod. 72, 1395-8, (2009)
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Chemical Constituents of the Roots of Euphorbia micractina. Wendong Xu et al J. Nat. Prod. 72, 1620-6, (2009)
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Rational design and semisynthesis of betulinic acid analogues as potent topoisomerase inhibitors. Fatma M Abdel Bar et al J. Nat. Prod. 72, 1643-50, (2009)
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Asterolaurins A-F, xenicane diterpenoids from the Taiwanese soft coral Asterospicularia laurae. Yu-Chi Lin et al J. Nat. Prod. 72, 1911-6, (2009)
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Cytotoxic xanthone constituents of the stem bark of Garcinia mangostana (mangosteen). Ah-Reum Han et al J. Nat. Prod. 72, 2028-31, (2009)
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Chemical constituents of the bark of Machilus wangchiana and their biological activities. Wei Cheng et al J. Nat. Prod. 72, 2145-52, (2009)
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Calothrixins, a new class of human DNA topoisomerase I poisons. Qasim A Khan et al J. Nat. Prod. 72, 438-42, (2009)
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Cytotoxic oleanane triterpene saponins from Albizia chinensis. Rui Liu et al J. Nat. Prod. 72, 632-9, (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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A series of alpha-amino acid ester prodrugs of camptothecin: in vitro hydrolysis and A549 human lung carcinoma cell cytotoxicity. Manjeet Deshmukh et al J. Med. Chem. 53, 1038-47, (2010)
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Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors. Yunlong Song et al J. Med. Chem. 53, 1979-89, (2010)
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Synthesis and antiproliferative evaluation of certain indeno[1,2-c]quinoline derivatives. Part 2. Chih-Hua Tseng et al J. Med. Chem. 53, 6164-79, (2010)
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Selection of evodiamine as a novel topoisomerase I inhibitor by structure-based virtual screening and hit optimization of evodiamine derivatives as antitumor agents. Guoqiang Dong et al J. Med. Chem. 53, 7521-31, (2010)
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Synthesis and biological analysis of prostate-specific membrane antigen-targeted anticancer prodrugs. Kularatne, S. A.; et al. J. Med. Chem. 53, 7767, (2010)
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New diterpenoids from Caesalpinia species and their cytotoxic activity. Biswanath Das et al Bioorg. Med. Chem. Lett. 20, 2847-50, (2010)
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2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study. Arjun Basnet et al Bioorg. Med. Chem. Lett. 20, 42-7, (2010)
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Oxidative stimuli-responsive nanoprodrug of camptothecin kills glioblastoma cells. Bong-Seop Lee et al Bioorg. Med. Chem. Lett. 20, 5262-8, (2010)
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New benzoxanthone derivatives as topoisomerase inhibitors and DNA cross-linkers. Hee-Ju Cho et al Bioorg. Med. Chem. 18, 1010-7, (2010)
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Synthesis of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship. Pritam Thapa et al Bioorg. Med. Chem. 18, 2245-54, (2010)
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Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines. Radha Karki et al Bioorg. Med. Chem. 18, 3066-77, (2010)
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Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities. Zhenyuan Miao et al Bioorg. Med. Chem. 18, 3140-6, (2010)
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2-Thienyl-4-furyl-6-aryl pyridine derivatives: synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study. Pritam Thapa et al Bioorg. Med. Chem. 18, 377-86, (2010)
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Synthesis and structure-activity relationship study of novel cytotoxic carbamate and N-acylheterocyclic bearing derivatives of betulin and betulinic acid. Rita C Santos et al Bioorg. Med. Chem. 18, 4385-96, (2010)
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Synthesis and antiproliferative evaluation of certain iminonaphtho[2,3-b]furan derivatives. Chih-Hua Tseng et al Bioorg. Med. Chem. 18, 5172-82, (2010)
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The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode. Maris A Cinelli et al Bioorg. Med. Chem. 18, 5535-52, (2010)
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Rubiyunnanins C-H, cytotoxic cyclic hexapeptides from Rubia yunnanensis inhibiting nitric oxide production and NF-?B activation. Jun-Ting Fan et al Bioorg. Med. Chem. 18, 8226-34, (2010)
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A diazirine-based photoaffinity etoposide probe for labeling topoisomerase II. Gaik-Lean Chee et al Bioorg. Med. Chem. 18, 830-8, (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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Synthesis and biological evaluation of new camptothecin derivatives obtained by modification of position 20. Elena Riva et al Bioorg. Med. Chem. 18, 8660-8, (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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Cytotoxicity and topo I targeting activity of substituted 10--nitrogenous heterocyclic aromatic group derivatives of SN-38. Qing-Yong Li et al Eur. J. Med. Chem. 45, 3200-6, (2010)
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Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors. De-Qing Shen et al Eur. J. Med. Chem. 45, 3938-42, (2010)
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Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues. Sangwook Woo et al Eur. J. Med. Chem. 45, 4221-8, (2010)
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Antifungal and cytotoxic activity of withanolides from Acnistus arborescens. Vincent Roumy et al J. Nat. Prod. 73, 1313-7, (2010)
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Cylindrocyclophanes with proteasome inhibitory activity from the Cyanobacterium Nostoc sp. George E Chlipala et al J. Nat. Prod. 73, 1529-37, (2010)
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Isolation and characterization of minor analogues of silvestrol and other constituents from a large-scale re-collection of Aglaia foveolata. Li Pan et al J. Nat. Prod. 73, 1873-8, (2010)
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Abietane and C20-norabietane diterpenes from the stem bark of Fraxinus sieboldiana and their biological activities. Sheng Lin et al J. Nat. Prod. 73, 1914-21, (2010)
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Cytotoxic activities of several geranyl-substituted flavanones. Karel Smejkal et al J. Nat. Prod. 73, 568-72, (2010)
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Humulane and germacrane sesquiterpenes from Ferula lycia. Racha Alkhatib et al J. Nat. Prod. 73, 780-3, (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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14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment. Jian-Xin Duan et al J. Med. Chem. 54, 1715-23, (2011)
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Structural simplification of bioactive natural products with multicomponent synthesis. 3. Fused uracil-containing heterocycles as novel topoisomerase-targeting agents. Nikolai M Evdokimov et al J. Med. Chem. 54, 2012-21, (2011)
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Discovery and preclinical evaluation of a novel class of cytotoxic propynoic acid carbamoyl methyl amides (PACMAs). Roppei Yamada et al J. Med. Chem. 54, 2902-14, (2011)
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Discovery of 4-anilinofuro[2,3-b]quinoline derivatives as selective and orally active compounds against non-small-cell lung cancers. Yu-Wen Chen et al J. Med. Chem. 54, 4446-61, (2011)
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Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity. Katherine E Peterson et al J. Med. Chem. 54, 4937-53, (2011)
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7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents. Evgeny Kiselev et al J. Med. Chem. 54, 6106-16, (2011)
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Improving anticancer activity and selectivity of camptothecin through conjugation with releasable substance P. Wei Zhang et al Bioorg. Med. Chem. Lett. 21, 1452-5, (2011)
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Synthesis and topoisomerase II inhibitory and cytotoxic activity of oxiranylmethoxy- and thiiranylmethoxy-chalcone derivatives. Younghwa Na et al Bioorg. Med. Chem. Lett. 21, 211-4, (2011)
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Synthesis of polyfunctionalized piperidone oxime ethers and their cytotoxicity on HeLa cells. Paramasivam Parthiban et al Bioorg. Med. Chem. Lett. 21, 6678-86, (2011)
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Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase I inhibitors. Daulat Bikram Khadka et al Bioorg. Med. Chem. 19, 1924-9, (2011)
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Design and synthesis of 4-amino-2-phenylquinazolines as novel topoisomerase I inhibitors with molecular modeling. Thanh Nguyen Le et al Bioorg. Med. Chem. 19, 4399-404, (2011)
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In vitro cytotoxic activity of abietane diterpenes from Peltodon longipes as well as Salvia miltiorrhiza and Salvia sahendica. M Fronza et al Bioorg. Med. Chem. 19, 4876-81, (2011)
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Synthesis of benzo[3,4]azepino[1,2-b]isoquinolin-9-ones from 3-arylisoquinolines via ring closing metathesis and evaluation of topoisomerase I inhibitory activity, cytotoxicity and docking study. Hue Thi My Van et al Bioorg. Med. Chem. 19, 5311-20, (2011)
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Cytotoxicity and topoisomerase I/II inhibition of glycosylated 2-phenyl-indoles, 2-phenyl-benzo[b]thiophenes and 2-phenyl-benzo[b]furans. Wei Shi et al Bioorg. Med. Chem. 19, 603-12, (2011)
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Design, synthesis, and biological evaluation of callophycin A and analogues as potential chemopreventive and anticancer agents. Li Shen et al Bioorg. Med. Chem. 19, 6182-95, (2011)
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Quinoline tricyclic derivatives. Design, synthesis and evaluation of the antiviral activity of three new classes of RNA-dependent RNA polymerase inhibitors A. Carta, et al., Bioorg. Med. Chem. 19, 7070-7084, (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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3-Arylisoquinolines as novel topoisomerase I inhibitors. Daulat Bikram Khadka et al Bioorg. Med. Chem. 19, 724-34, (2011)
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Camptothecin (CPT) directly binds to human heterogeneous nuclear ribonucleoprotein A1 (hnRNP A1) and inhibits the hnRNP A1/topoisomerase I interaction. Daisuke Manita et al Bioorg. Med. Chem. 19, 7690-7, (2011)
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A comparative study of proapoptotic potential of cyano analogues of boswellic acid and 11-keto-boswellic acid. Rajbir Kaur et al Eur. J. Med. Chem. 46, 1356-66, (2011)
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Synthesis, biological evaluation, and molecular docking study of 3-(3'-heteroatom substituted-2'-hydroxy-1'-propyloxy) xanthone analogues as novel topoisomerase II? catalytic inhibitor. Kyu-Yeon Jun et al Eur. J. Med. Chem. 46, 1964-71, (2011)
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Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents. Constance Genès et al Eur. J. Med. Chem. 46, 2117-31, (2011)
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Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors. Wenfeng Liu et al Eur. J. Med. Chem. 46, 2408-14, (2011)
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Synthesis and antiproliferative activity of novel symmetrical alkylthio- and alkylseleno-imidocarbamates. Elena Ibáñez et al Eur. J. Med. Chem. 46, 265-74, (2011)
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Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship. Uttam Thapa et al Eur. J. Med. Chem. 46, 3201-9, (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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Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors. Wei-Bin Wu et al Eur. J. Med. Chem. 46, 3339-47, (2011)
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6-Substituted imidazo[1,2-a]pyridines: synthesis and biological activity against colon cancer cell lines HT-29 and Caco-2. Nurit Dahan-Farkas et al Eur. J. Med. Chem. 46, 4573-83, (2011)
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Synthesis and biological activity of novel inhibitors of topoisomerase I: 2-aryl-substituted 2-bis-1H-benzimidazoles. Manish Singh et al Eur. J. Med. Chem. 46, 659-69, (2011)
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Resorcylic acid lactones with cytotoxic and NF-?B inhibitory activities and their structure-activity relationships. Sloan Ayers et al J. Nat. Prod. 74, 1126-31, (2011)
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Kabiramides J and K, trisoxazole macrolides from the sponge Pachastrissa nux. Thanchanok Sirirak et al J. Nat. Prod. 74, 1288-92, (2011)
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Spirocyclic lignans from Guaiacum (Zygophyllaceae) induce apoptosis in human breast cancer cell lines. Kathryn J Chavez et al J. Nat. Prod. 74, 1293-7, (2011)
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Biologically active arborinane-type triterpenoids and anthraquinones from Rubia yunnanensis. Jun-Ting Fan et al J. Nat. Prod. 74, 2069-80, (2011)
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Structure and in vitro antiparasitic activity of constituents of Citropsis articulata root bark. Damien Lacroix et al J. Nat. Prod. 74, 2286-9, (2011)
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Cucurbitane glucosides from the root of Machilus yaoshansis. Maoluo Gan et al J. Nat. Prod. 74, 2431-7, (2011)
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Symmetric dimers of ent-kaurane diterpenoids with cytotoxic activity from Croton tonkinensis. Phuong Thien Thuong et al Bioorg. Med. Chem. Lett. 22, 1122-4, (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 biological evaluation of 4?-sulphonamido and 4?-[(4'-sulphonamido)benzamide]podophyllotoxins as DNA topoisomerase-II? and apoptosis inducing agents. Ahmed Kamal et al Bioorg. Med. Chem. 20, 2054-66, (2012)
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Sulfur and selenium derivatives of quinazoline and pyrido[2,3-d]pyrimidine: synthesis and study of their potential cytotoxic activity in vitro. Esther Moreno et al Eur. J. Med. Chem. 47, 283-98, (2012)
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Design, synthesis and biological evaluation of new naphtalene diimides bearing isothiocyanate functionality. Anna Minarini et al Eur. J. Med. Chem. 48, 124-31, (2012)
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Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study. Radha Karki et al Eur. J. Med. Chem. 49C, 219-28, (2012)
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Synthesis of chromeno[3,4-b]indoles as Lamellarin D analogues : A novel DYRK1A inhibitor class. Cleopatra Neagoie et al Eur. J. Med. Chem. 49C, 379-96, (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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Hybrids of privileged structures benzothiazoles and pyrrolo[2,1-c] [1,4]benzodiazepin-5-one, and diversity-oriented synthesis of benzothiazoles. D Subhas Bose et al Eur. J. Med. Chem. 50, 27-38, (2012)
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Merck 14,1735
FT-IR 2 (3), 4267:D / Structure Index 1, 462:C:1