Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives

K Nakagawa-Goto, CX Chen, E Hamel, CC Wu…

Index: Nakagawa-Goto, Kyoko; Chen, Cyril X.; Hamel, Ernest; Wu, Chin-Chung; Bastow, Kenneth F.; Brossi, Arnold; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 1 p. 235 - 238

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Citation Number: 29

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 IC50 values ranging from 0.02 to 0.88 μg/mL. The thiocolchicine analogs (5, 5a) were more potent than ...