Imidazolone–amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: Synthesis and biological evaluation
Abstract A series of novel combretastatin-A4 analogues in which the cis-olefinic bridge is replaced by an imidazolone–amide were synthesized, and their cytotoxicity and tubulin- polymerization inhibitory activities were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors. Compounds 10, 9b and 9c, bearing 3′-NH 2-4′-OCH 3, 4′-CH 3 and 3′-CH 3-substituted 1-phenyl B-ring, confer optimal bioactivity. The ...
