期刊
ARCHIV DER PHARMAZIE
卷 347, 期 9, 页码 658-667出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201400096
关键词
Cytotoxicity; Docking study; 1; 2; 4-Triazole; Tubulin
资金
- Science and Technology Development Fund (STDF) Egypt [2943]
A series of novel 1-(3,4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxylic acid derivatives (4a-n) were synthesized and evaluated for their in vitro cytotoxic activity against the growth of four different human cell lines (hepatocarcinoma HepG2, breast adenocarcinoma MCF-7, colon carcinoma DLD-1, and leukemia HL-60). The anilides of m-anisidine 4e, o-anisidine 4f, and 3,5-difluoroaniline 4l demonstrated best results on MCF-7 cells and mean IC50 values of 7.79, 10.79, and 13.20 mu M, respectively. The compounds produced a significant reduction in cellular microtubules at a concentration of 25 mu g/mL, for microtubule loss. Molecular modeling studies involving compounds 4d, 4e, 4f, and 4l with the colchicine binding site of ,-tubulin revealed hydrogen bonding and hydrophobic interactions with several amino acids in the colchicine binding site of beta-tubulin.
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