- Analogues and derivatives of oncrasin-1, a novel inhibitor of the C-terminal domain of RNA polymerase II and their antitumor activities
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To optimize the antitumor activity of oncrasin-1, a small molecule RNA polymerase II inhibitor, we evaluated 69 oncrasin-1 analogues for their cytotoxic activity against normal human epithelial cells and K-Ras mutant tumor cells. About 40 of those compoun
- Wu, Shuhong,Wang, Li,Guo, Wei,Liu, Xiaoying,Liu, Jinsong,Wei, Xiaoli,Fang, Bingliang
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experimental part
p. 2668 - 2679
(2011/06/27)
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- Synthesis and antifungal activity of new 1-halogenobenzyl-3-imidazolylmethylindole derivatives
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A series of 1-benzyl-3-(imidazol-1-ylmethyl)indole derivatives 35-46 were prepared under mild reaction conditions and tested for their antifungal activity. Pharmacomodulation at N1, C2 and C5 of the indole ring and at the level of the alkyl chain (R1) was carried out starting from the corresponding 3-acylindoles 6, 7 or 3-formylindoles 11-22. Target imidazolyl compounds 35-46 were obtained in satisfactory yields by CO2 elimination from the intermediate carbamates. All of the compounds were evaluated in vitro against two human fungal pathogens, Candida albicans (CA980001) and Aspergillus fumigatus (AF980003); amphotericin B, fluconazole and itraconazole were used as references. Seven out of 27 compounds (35b, 35e, 35g, 35h, 36a, 38a and especially 40a) exerted significant antifungal activity against C. albicans, with MIC in the range of 1-6 μg mL-1. As regards inhibitory activity against A. fumigatus, the MIC figures of most of our compounds were in excess of 20 μg mL-1 in contrast to the reference drugs, amphotericin B and itraconazole, whose MIC90 and MIC80 values were 0.14 and 0.50 μg mL-1, respectively. The most potent compound, 45a, exhibited MIC value (8±1 μg mL-1) 16-fold higher than that of itraconazole.
- Na, Young-Min,Le Borgne, Marc,Pagniez, Fabrice,Le Baut, Guillaume,Le Pape, Patrice
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- Syntheses and in vitro antimycotic activities of 1-benzyl-3-(1-imidazolylmethyl)indoles
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Syntheses of seventeen 1-benzyl-3-(1-imidazolylmethyl)indoles with substituents at the benzyl moiety and at the indole C-2 position are described. The compounds were tested for their antifungal activities in vitro determination of the minimum inhibitory concentration (MIC). Three compounds exhibited appreciable activities against Cr. neoformans.
- Cavrini,Gatti,Roveri,Cesaroni,Mazzoni,Fiorentini
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p. 662 - 668
(2007/10/02)
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