期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 22, 页码 5757-5762出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.08.087
关键词
cytotoxicity; combretastatin A-4; colchicine; imidazoles; tubulin; molecular modeling; antitumor activity
The in vitro antitumor activity of novel combretastatin-like 1,5- and 1,2-diaryl-1H-imidazoles was evaluated against the NCI 60 human tumor cell lines panel. Compounds 2d and 2g proved to be more cytotoxic than CA-4 in tests involving their evaluation over a 10(-4)-10(-8) range. Docking experiments showed a good correlation between the MG_MID Log GI(50) values of all these compounds and their calculated interaction energies with the colchicine binding site of alpha beta-tubulin. (c) 2006 Elsevier Ltd. All rights reserved.
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