Synthesis and Biological Evaluation of 2-(3’,4’,5’-Trimethoxybenzoyl)-3-N,N-Dimethylamino Benzo[b]furan Derivatives as Inhibitors of Tubulin Polymerization

Mols. that target microtubules have an important role in the treatment of cancer. A new class of inhibitors of tubulin polymn. based on the 2-(3,4,5-trimethoxybenzoyl)-2-dimethylamino-benzo[b]furan mol. skeleton was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymn., and cell cycle effects. The most promising compd. in this series was 2-(3,4,5-trimethoxybenzoyl)-3-dimethylamino-6-methoxy-benzo[b]furan, which inhibits cancer cell growth at nanomolar concns. and interacts strongly with tubulin by binding to the colchicine site.