Original Articles: 2013 Vol: 5 Issue: 12
Design, synthesis and biological evaluation of 3-benzylidene 4-bromo isatin derivatives
Abstract
4-Bromo substitution on isatin based molecules has been found to increase their cytotoxic activity and selectivity. So the studies on synthesis and pharmacological activities of 4-Bromo isatin and its derivatives have been attracted more and more attention. In this paper, we would like to report the design, synthesis and biological evaluation of a series of 3-benzylidene 4-Bromo isatin derivatives. Eight 3-benzylidene 4-bromo isatin derivatives were designed and synthesized in 4 steps in 44-75% overall yields. Six of the eight newly synthesized compounds have not been reported before. Their structures were characterized by 1H-NMR. The anticancer activity of these new 4-Bromo isatin derivatives against two human tumor cell lines, K562 and HepG2, were evaluated by MTT assay in vitro. MTT results suggests that larger groups at the 3-position could increase the antitumor potency