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Simon B Cammerer et al.
Antimicrobial agents and chemotherapy, 51(11), 4049-4061 (2007-08-22)
There is an urgent need for the development of new drugs for the treatment of tropical parasitic diseases such as Chagas' disease and leishmaniasis. One potential drug target in the organisms that cause these diseases is sterol biosynthesis. This paper
Gang Feng et al.
Natural product communications, 8(2), 199-202 (2013-03-22)
To continue our search for natural product-based compounds for the control of Brontispa longissima larvae, eight spin-labeled podophyllotoxin derivatives (4a-h) and the intermediates 2 and 3 were tested for their insect antifeedant activity against third-instar larvae of B. longissima. Among
Stanislav A Bakunov et al.
Journal of medicinal chemistry, 53(1), 254-272 (2009-11-26)
Novel dicationic triazoles 1-60 were synthesized by the Pinner method from the corresponding dinitriles, prepared via the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC). The type and the placement of cationic moieties as well as the nature of aromatic substituents influenced in vitro
Abdelhalim Babiker Mahmoud et al.
Frontiers in pharmacology, 11, 1246-1246 (2020-09-15)
In a screening of Sudanese medicinal plants for antiprotozoal activity, the chloroform fractions obtained by liquid-liquid partitioning from ethanolic extracts of fruits of Croton gratissimus var. gratissimus and stems of Cuscuta hyalina Roth ex Schult. exhibited in vitro activity against
Fadoua Bouchikhi et al.
Bioorganic & medicinal chemistry letters, 21(21), 6319-6321 (2011-09-23)
The biological activities of diversely substituted glycosyl-isoindigo derivatives against the causative agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis) are reported. Some of the compounds tested showed interesting activities with good selectivity indices, particularly against Trypanosoma
Beatriz Baragaña et al.
Bioorganic & medicinal chemistry, 19(7), 2378-2391 (2011-03-18)
We report a series of β-branched acyclic tritylated deoxyuridine analogues as inhibitors of Plasmodium falciparum deoxyuridine-5'-triphosphate nucleotidohydrolase (PfdUTPase), an enzyme involved in nucleotide metabolism that acts as first line of defence against uracil incorporation into DNA. Compounds were assayed against
Siavosh Mahboobi et al.
Journal of medicinal chemistry, 49(19), 5769-5776 (2006-09-15)
Synthesis and cytotoxic activity in the submicromolar range of a series of [4-(imidazol-1-yl)thiazol-2-yl]phenylamines are described. Cell cycle dependent cytotoxicity on RKO human colon carcinoma cells with inducible expression of p27(kip1) and the influence on microtubule formation were investigated. Considering the
Hari Om Saxena et al.
Bioorganic & medicinal chemistry letters, 18(14), 3914-3918 (2008-07-01)
Gallic acid-based indanone derivatives have been synthesised. Some of the indanones showed very good anticancer activity in MTT assay. Compounds 10, 11, 12 and 14 possessed potent anticancer activity against various human cancer cell lines. The most potent indanone (10
Gerhard Bringmann et al.
European journal of medicinal chemistry, 45(11), 5370-5383 (2010-09-21)
Naphthylisoquinoline alkaloids have attracted considerable interest because of their intriguing structure, their unique biosynthetic origin, and their biological activities against several pathogens causing tropical diseases. Their promising pharmacologic properties make them suitable lead structures for new agents, in particular against
Stephen T McCracken et al.
Bioorganic & medicinal chemistry, 20(4), 1482-1493 (2012-01-31)
Previous studies have identified the 3,6-dialkyl-4-hydroxy-pyran-2-one marine microbial metabolites pseudopyronines A and B to be modest growth inhibitors of Mycobacterium tuberculosis and a range of tropical diseases including Plasmodium falciparum and Leishmania donovani. In an effort to expand the structure-activity
Van Trinh Thi Thanh et al.
Journal of natural products, 75(9), 1578-1583 (2012-09-04)
Two new aryl-tetralin lignans, 1 and 2, were isolated from the fruits of Cleistanthus indochinensis by bioassay-guided purification. Their structures were determined by spectroscopic analysis including MS and 2D NMR. The absolute configurations of 1 and 2 were established from
Jennifer Keiser et al.
The Journal of antimicrobial chemotherapy, 70(6), 1788-1797 (2015-02-19)
Praziquantel is the only drug available for the treatment of schistosomiasis and the state of the exhausted drug discovery pipeline is alarming. We restarted investigations on the abandoned antischistosomal Ro 13-3978, an aryl hydantoin discovered in the early 1980s by
Zhigang Wu et al.
PloS one, 8(3), e57642-e57642 (2013-03-08)
Conbercept is a genetically engineered homodimeric protein for the treatment of wet age-related macular degeneration (wet AMD) that functions by blocking VEGF-family proteins. Its huge, highly variable architecture makes characterization and development of a functional assay difficult. In this study
Pawan Kumar et al.
Protoplasma, 252(5), 1253-1262 (2015-01-15)
Podophyllum hexandrum Royle is known for its vast medicinal properties, particularly anticancer. It contains higher amount of podophyllotoxin (4.3 %), compared to Podophyllum peltatum (0.025 %) and other plant species; as a result, it has been used worldwide in the
Ma Angeles Castro et al.
Journal of medicinal chemistry, 53(3), 983-993 (2010-01-14)
Several series of nonlactonic podophyllic aldehyde analogues were prepared and evaluated against several human tumor cell lines. They had different combinations of aldehyde, imine, amine, ester, and amide functions at C-9 and C-9' of the cyclolignan skeleton. All the compounds
Grushenka H I Wolfgang et al.
Antimicrobial agents and chemotherapy, 53(7), 2777-2784 (2009-04-29)
GS-9191 is a novel double prodrug of the nucleotide analog 9-(2-phosphonylmethoxyethyl)guanine (PMEG) designed as a topical agent to permeate skin and be metabolized to the active nucleoside triphosphate analog in the epithelial layer. The prodrug was shown to be metabolized
Wendy Itzel Escobedo Hinojosa et al.
Journal of ethnopharmacology, 155(2), 1156-1163 (2014-06-28)
The root barks of Hippocratea celastroides have been used for decades in Mexican traditional medicine to treat gastritis and ulcers. To investigate the anti-Helicobacter pylori, gastroprotective, anti-inflammatory, and cytotoxic activities of methanolic extracts obtained from the leaves, stems, and root
Brittany Lee et al.
Journal of medicinal chemistry, 48(23), 7400-7410 (2005-11-11)
Trypanothione reductase is a flavoenzyme unique to trypanosomatid parasites. Here we show that unsaturated Mannich bases irreversibly inactivate trypanothione reductase from Trypanosoma cruzi, the causative agent of Chagas' disease. The inhibitory potency of the compounds strongly increased upon storage of
Ahmed Kamal et al.
Bioorganic & medicinal chemistry letters, 21(1), 350-353 (2010-12-15)
An efficient one-pot iodination methodology for the synthesis of benzothiazolo-4β-anilino-podophyllotoxin (5a-h) and benzothiazolo-4β-anilino-4-O-demethylepipodophyllotoxin (6a-h) congeners has been successfully developed by using zirconium tetrachloride/sodium iodide. Interestingly, this protocol demonstrates enhancement of stereoselectivity apart from the improvement in the yields in comparison
Renu Mohan et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(22), 8900-8905 (2013-05-16)
Microtubule-targeting agents (MTAs) are widely used for treatment of cancer and other diseases, and a detailed understanding of the mechanism of their action is important for the development of improved microtubule-directed therapies. Although there is a large body of data
The chemical and biological route from podophyllotoxin glucoside to etoposide: ninth Cain memorial Award lecture.
H F Stähelin et al.
Cancer research, 51(1), 5-15 (1991-01-01)
Podophyllotoxin derivatives VP-16 and VM-26.
M D'Incalci et al.
Cancer chemotherapy and biological response modifiers, 9, 67-70 (1987-01-01)
Alex S Kiselyov et al.
European journal of medicinal chemistry, 45(5), 1683-1697 (2010-01-30)
A series of novel 1,3,4-oxadiazole derivatives based on structural and electronic overlap with combretastatins have been designed and synthesized. Initially, we tested all new compounds in vivo using the phenotypic sea urchin embryo assay to yield a number of agents
Simon M N Efange et al.
Journal of natural products, 72(2), 280-283 (2009-02-10)
Okundoperoxide (1) was isolated by bioassay-guided fractionation of extracts from Scleria striatinux (syn. S. striatonux). The compound contains a cyclic endoperoxide structural moiety and possesses moderate antimalarial activity.
Podophyllotoxin derivatives VP-16 and VM-26.
M D'Incalci et al.
Cancer chemotherapy and biological response modifiers, 10, 57-63 (1988-01-01)
Kuo-Hsiung Lee
Journal of natural products, 73(3), 500-516 (2010-03-02)
Medicinal plants have long been an excellent source of pharmaceutical agents. Accordingly, the long-term objectives of the author's research program are to discover and design new chemotherapeutic agents based on plant-derived compound leads by using a medicinal chemistry approach, which
Zhi Yang et al.
Journal of separation science, 36(6), 1022-1028 (2013-02-19)
Dysosma versipellis (Hance) is a famous traditional Chinese medicine for the treatment of snakebite, weakness, condyloma accuminata, lymphadenopathy, and tumors for thousands of years. In this work, four podophyllotoxin-like lignans including 4'-demethylpodophyllotoxin (1), α-peltatin (2), podophyllotoxin (3), β-peltatin (4) as
Peter Nussbaumer et al.
Bioorganic & medicinal chemistry, 16(16), 7552-7560 (2008-08-06)
The potent antiproliferative agent SDZ LAP 977, which has shown efficacy in a clinical proof of concept study in actinic keratosis patients, has been previously demonstrated to block the cell cycle in mitosis. In the present study, we further explored
Amy L Eyberger et al.
Journal of natural products, 69(8), 1121-1124 (2006-08-29)
The lignan podophyllotoxin (1) is highly valued as the precursor to clinically useful anticancer drugs. Substantial drug development of this compound class continues, including potential new use for inflammatory disease. We have isolated two endophyte fungi, both strains of Phialocephala
Ma Angeles Castro et al.
Bioorganic & medicinal chemistry, 15(4), 1670-1678 (2007-01-02)
A series of podophyllotoxin and podophyllic aldehyde derivatives, lacking the lactone ring and oxidized at C-9 position, has been prepared. The functionalities considered at C-9 were carboxylic acids and several derivatives such as esters, amides, nitriles or anhydrides. The synthesized
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