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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
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
Seong-Jin Kim et al.
Theranostics, 10(18), 7974-7992 (2020-07-30)
Breast cancer (BC) is one of the most common cancers in women. TNBC (Triple-negative breast cancer) has limited treatment options and still lacks viable molecular targets, leading to poor outcomes. Recently, RNA-binding proteins (RBPs) have been shown to play crucial
Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities.
Petritsch, et al.
European Journal of Medicinal Chemistry, 210, 112969-112969 (2021)
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
Kathleen Too et al.
Bioorganic & medicinal chemistry, 15(16), 5551-5562 (2007-06-06)
Plasmodium falciparum causes one of the deadliest forms of malaria and resistance to the currently available drugs makes it imperative to develop new, safe and potent drugs. Parasites such as P. falciparum are unable to synthesise purines de novo and
Deniz Tasdemir et al.
Bioorganic & medicinal chemistry, 18(21), 7475-7485 (2010-09-22)
Acetylenic fatty acids are known to display several biological activities, but their antimalarial activity has remained unexplored. In this study, we synthesized the 2-, 5-, 6-, and 9-hexadecynoic acids (HDAs) and evaluated their in vitro activity against erythrocytic (blood) stages
Manar M Salem et al.
Journal of natural products, 69(1), 43-49 (2006-01-31)
Bioactivity-guided fractionation of the root extract of Psorothamnus arborescens yielded the new isoflavone 5,7,3',4'-tetrahydroxy-2'-(3,3-dimethylallyl)isoflavone (1a) and the new 2-arylbenzofuran 2-(2'-hydroxy-4',5'-methylenedioxyphenyl)-6-methoxybenzofuran-3-carbaldehyde (2), together with seven known compounds, including three isoflavones, fremontin (3a), glycyrrhisoflavone (4a), and calycosin (5), two pterocarpans, maackiain (6)
Susanna T S Chan et al.
Journal of natural products, 74(9), 1972-1979 (2011-08-19)
One tetrahydro-β-carboline, (-)-7-bromohomotrypargine (1), and three alkylguanidine-substituted β-carbolines, opacalines A, B, and C (2-4), have been isolated from the New Zealand ascidian Pseudodistoma opacum. The structures of the metabolites were determined by analysis of mass spectrometric and 2D NMR spectroscopic
Ronald W Brown et al.
RSC medicinal chemistry, 11(12), 1413-1422 (2021-06-08)
African sleeping sickness is a potentially fatal neglected disease affecting sub-Saharan Africa. High-throughput screening identified the thiazolyl-benzothiophenamide 1 to be active against the causative parasite, Trypanosoma brucei. This work establishes structure-activity relationships of 1, guiding the design of second generation
Vasudeva Rao Avupati et al.
Bioorganic & medicinal chemistry letters, 22(2), 1031-1035 (2011-12-28)
A series of novel diarylsulfonylureas (1-28) have been synthesized and characterized by FTIR, (1)H NMR, (13)C NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their in vitro cytotoxicity and antimicrobial activities. Among the tested compounds
Ran Rostoker et al.
Endocrinology, 154(5), 1701-1710 (2013-03-22)
Epidemiological and experimental studies have identified hyperinsulinemia as an important risk factor for breast cancer induction and for the poor prognosis in breast cancer patients with obesity and type 2 diabetes. Recently it was demonstrated that both the insulin receptor
Jyothi Vantikommu et al.
European journal of medicinal chemistry, 45(11), 5044-5050 (2010-09-14)
A facile and highly efficient method for the regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles (β-keto 1,2,3-triazoles) in good to excellent yields from in-situ generated β-ketoazides and terminal alkynes through Cu(I) catalyzed 1,3 dipolar cycloaddition is described. This reaction proceeds smoothly either
Gerhard Bringmann et al.
European journal of medicinal chemistry, 43(1), 32-42 (2007-05-04)
The naphthylisoquinoline alkaloids (NIQs) represent a class of natural products with manifold activities against various tropical diseases. They are isolated from rare and difficult-to-cultivate tropical plants. In order to find novel, more easily accessible analogs and to study structure-activity relationships
Laixing Hu et al.
Bioorganic & medicinal chemistry letters, 17(13), 3613-3617 (2007-05-08)
We report the synthesis, antiproliferative activity, and SAR of novel heterocyclic ketones derived from carbazole sulfonamides. Most of the heterocyclic ketones showed strong cytotoxicities. (N-1-Methylindole-5-yl)-(3,4,5-trimethoxyphenyl)-methanone 8b gave the most potent cytotoxicity (9.2-26 nM) against seven human tumor cell lines. The
Gerhard Bringmann et al.
Journal of medicinal chemistry, 50(24), 6104-6115 (2007-11-10)
The naphthylisoquinoline (NIQ) alkaloids from tropical Ancistrocladaceae and Dioncophyllaceae plants show high antiplasmodial activities in vitro and in vivo, even against chloroquine-resistant strains of the malaria pathogen. For the directed optimization of these activities, an investigation of the mode of
Martin Senn et al.
Journal of natural products, 70(10), 1565-1569 (2007-10-10)
From the petroleum ether extract of the root bark of Cussonia zimmermannii four polyacetylenes, 1- 4, were isolated, three of which ( 1- 3) were active against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Plasmodium falciparum, and Leishmania donovani.
Igor V Magedov et al.
Journal of medicinal chemistry, 54(12), 4234-4246 (2011-05-28)
Structural simplification of an antimitotic natural product podophyllotoxin with mimetic heterocyclic scaffolds constructed using multicomponent reactions led to the identification of compounds exhibiting low nanomolar antiproliferative and apoptosis-inducing properties. The most potent compounds were found in the dihydropyridopyrazole, dihydropyridonaphthalene, dihydropyridoindole
Podophyllotoxin derivatives VP-16 and VM-26.
M D'Incalci et al.
Cancer chemotherapy and biological response modifiers, 10, 57-63 (1988-01-01)
Abdelhalim Babiker Mahmoud et al.
Molecules (Basel, Switzerland), 25(12) (2020-06-25)
A screening of Sudanese medicinal plants for antiprotozoal activities revealed that the chloroform and water fractions of the ethanolic root extract of Haplophyllum tuberculatum exhibited appreciable bioactivity against Leishmania donovani. The antileishmanial activity was tracked by HPLC-based activity profiling, and
Yaşar Dürüst et al.
European journal of medicinal chemistry, 48, 296-304 (2012-01-06)
1,2,4-Oxadiazole and 1,2,3-triazole containing heterocyclic compounds continue to gain interest in synthesis of chemical entities and exhibit various biological activities as anti-protozoal and anti-cancer agents. By using the principle of bioisosterism, a series of novel oxadiazolyl pyrrolo triazole diones; namely
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
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
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.
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
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
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
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
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
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