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Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
来源: 时间:2014-07-08 浏览次数:3223
Eur J Med Chem. 2013 Jul;65:187-94. doi: 10.1016/j.ejmech.2013.04.046. Epub 2013 May 2.
Synthesis and antitumoractivity of novel3,4-diarylsquaricacid analogs.
  • Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, People's Republic of China.
Abstract
A series of novel 3,4-diaryl squaric acid analogs 4a-r related to combretastatin A-4 (CA4) using squaric acid as the cis-restricted linker were prepared and studied for their anticancer activity against selected human cancer cell lines. New compounds 4g, 4k, 4m, 4n, 4p, 4q and 4r exhibit strong activities against human leukemia cells with IC50 values of ≤20 nM and compounds 4k, 4n, 4p, 4q and 4r showed potent activities against a panel of human tumor cell lines. Compounds 4n and 4p arrest tumor cell cycle in G2-M phase. Computational modeling analysis suggests that the binding mechanism of compound 4n to the colchicine binding site on the microtubules is similar to that of CA4.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.
KEYWORDS:
3,4-Diaryl squaric acid analogs, Anticancer, Cytotoxic agents