| Literature DB >> 15582446 |
Kyoko Nakagawa-Goto1, Cyril X Chen, Ernest Hamel, Chin-Chung Wu, Kenneth F Bastow, Arnold Brossi, Kuo-Hsiung Lee.
Abstract
Water-soluble colchicine derivatives were synthesized from 2-demethylcolchicine and 2-demethylthiocolchicine and evaluated in vitro against human tumor cell replication and for inhibition of tubulin polymerization. The glycinate esters (4, 5) and their tartaric acid salts (4a, 5a) showed potent cytotoxic activity in three different tumor cell lines with IC(50) values ranging from 0.02 to 0.88 microg/mL. The thiocolchicine analogs (5, 5a) were more potent than the colchicine analogs (4, 4a) in the tubulin polymerization assay. In particular, the water-soluble salt 5a merits preclinical development as an antitumor agent.Entities:
Mesh：
Substances：
Year: 2005 PMID： 15582446 DOI： 10.1016/j.bmcl.2004.07.098
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823