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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
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
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
Joaquim V Marques et al.
The Journal of biological chemistry, 288(1), 466-479 (2012-11-20)
Podophyllum species are sources of (-)-podophyllotoxin, an aryltetralin lignan used for semi-synthesis of various powerful and extensively employed cancer-treating drugs. Its biosynthetic pathway, however, remains largely unknown, with the last unequivocally demonstrated intermediate being (-)-matairesinol. Herein, massively parallel sequencing of
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
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)
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
Podophyllotoxin derivatives VP-16 and VM-26.
M D'Incalci et al.
Cancer chemotherapy and biological response modifiers, 9, 67-70 (1987-01-01)
A Kruczynski et al.
Leukemia, 27(11), 2139-2148 (2013-04-10)
Chemotherapy remains mainly used for the treatment of acute myeloid leukemia (AML). However, in the past 3 decades limited progress has been achieved in improving the long-term disease-free survival. Therefore the development of more effective drugs for AML represents a
Laixing Hu et al.
Bioorganic & medicinal chemistry letters, 17(5), 1193-1196 (2007-01-02)
A series of azaheterocyclic carbazole sulfonamides was synthesized and evaluated for antiproliferative activity. The most potent compounds N-(2,6-dimethoxypyridine-3-yl)-9-ethyl and 9-methylcarbazole-3-sulfonamide (13 and 14) gave significant cytotoxicity (IC50 = 122 and 101 nM). Compound 13 displayed submicromolar activities against seven human
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
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)
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
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
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
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.
Alix O'Meara et al.
Biology of blood and marrow transplantation : journal of the American Society for Blood and Marrow Transplantation, 19(1), 82-86 (2012-08-18)
Allogeneic stem cell transplant (SCT) after high-dose conditioning with BEAM/fludarabine/total body irradiation (TBI) in patients with relapsed or refractory lymphoma has shown promising results in a pilot study. In this trial, we treated 50 consecutive patients with refractory or relapsed
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
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
Marc Steben et al.
Journal of lower genital tract disease, 17(2), 147-153 (2013-01-25)
We assessed temporal trend in the incidence and prevalence of genital warts (GWs) in the province of Quebec, Canada, between 1998 and 2007 as a baseline for future assessment of the impact of Quebec human papillomavirus vaccination program. Data on
Svetlana M Bakunova et al.
Journal of medicinal chemistry, 52(7), 2016-2035 (2009-03-10)
Diamidine 1 (pentamidine) and 65 analogues (2-66) have been tested for in vitro antiprotozoal activities against Trypanosoma brucei rhodesiense, Plasmodium falciparum, and Leishmania donovani, and for cytotoxicity against mammalian cells. Dications 32, 64, and 66 exhibited antitrypanosomal potencies equal or
M Salomé Gachet et al.
Journal of natural products, 74(4), 559-566 (2011-03-29)
In a survey of plants from Ecuador with antiprotozoal activity, Cupania cinerea was found to show significant in vitro activity against the Plasmodium falciparum K1 strain and Trypanosoma brucei rhodesiense. Subsequently, activity-guided isolation of the n-hexane and dichloromethane extracts from
Deniz Tasdemir et al.
Bioorganic & medicinal chemistry, 15(21), 6834-6845 (2007-09-04)
The type II fatty acid pathway (FAS-II) is a validated target for antimicrobial drug discovery. An activity-guided isolation procedure based on Plasmodium falciparum enoyl-ACP reductase (PfFabI) enzyme inhibition assay on the n-hexane-, the CHCl(3-) and the aq MeOH extracts of
Mehmet Alp et al.
European journal of medicinal chemistry, 44(5), 2002-2008 (2008-11-18)
A series of 2'-arylsubstituted-1H,1'H-[2,5']-bisbenzimidazolyl-5-carboxamidines were prepared in a six-step process starting from 4-amino-3-nitrobenzonitrile. The antiparasitic activity against Trypanosoma brucei rhodesiense (T.b.r.), Plasmodium falciparum (P.f.), Leishmania donovani (L.d.) and Trypanosoma cruzi (T.c.) and antifungal activity against Candida albicans and Candida krusei
Annie Mayence et al.
Bioorganic & medicinal chemistry, 19(24), 7493-7500 (2011-11-09)
A small library of 26 2,2'-[alkane-α,ω-diylbis(oxyphenylene)]bis-1H-benzimidazoles has been prepared and evaluated against Giardia intestinalis, Entamoeba histolytica, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum. Among the tested compounds, eight derivatives (17, 19, 20, 24, 27, 30, 32 and
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this
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
Shu-Cheng Yin et al.
Biochemical and biophysical research communications, 439(1), 1-5 (2013-08-27)
Insulin-like growth factor-1 receptor (IGF-1R) is a cell membrane receptor with tyrosine kinase activity and plays important roles in cell transformation, tumor growth, tumor invasion, and metastasis. Picropodophyllin (PPP) is a selective IGF-1R inhibitor and shows promising antitumor effects for
Ahmed Kamal et al.
Bioorganic & medicinal chemistry letters, 23(1), 273-280 (2012-11-28)
A series of different heteroaromatic linked 4β-amidopodophyllotoxin conjugates (16a-i, 17a-i and 18a-d) were synthesized and evaluated for anticancer activity against five human cancer cell lines. Among the series, one of the compound 17g showed significant antiproliferative activity in A549 (lung
Bochan Wang et al.
The American journal of Chinese medicine, 41(1), 163-175 (2013-01-23)
Podophyllotoxin, a kind of lignan extracted from the Podophyllum plant, has been shown to inhibit the growth of various carcinoma cells. However, the molecular mechanism remains unclear. In this study, the inhibition of cell growth and changes in protein expression
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