Design, synthesis and biological evaluation of 3-benzylidene 4-bromo isatin derivatives

作者：Zhou Yao; Shi Biao; Han Kailin; Guo Qiannan; Yang Yao; Song Binbin; Teng Yuou; Yu Peng

来源：Journal of Chemical and Pharmaceutical Research, 2013, 5(12): 1024-1028.

• Anti-tumor activities
• Anticancer activities
• Biological evaluation
• Human tumor cell lines
• Isatin derivatives
• K562
• MTT
• Pharmacological activity

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.

• 出版日期2013
• 单位天津大学