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 μg/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.
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