Design, synthesis, and biological evaluation of the novel antitumor agent 5-bromobenzofuran-3(2H)-One and its Derivatives

Abstract

Aurones and auronols are naturally occurring 2-benzylidenebenzof-uranone- 3(2H)-one derivatives. Aurones have a limited occurrence in fruits, vegetables, and bright yellow color to flowers such as cosmos and coreopsis. Aurones possess a wide range of biological activities, such as antitumor, antifungal, phytoalexin, and so on. Some aurone derivatives have been studied as antitumor drug molecules, but 2-benzylidene-5-bromobenzofuranone-3(2H)-one series have not been reported yet. In this paper, we'd like to report the design, synthesis, and biological evaluation of the novel aurone derivatives. All the newly synthesized compounds were characterized by 1H NMR and their antitumor activities were evaluated by using MTT method in HT-29, K562, and HepG2 cell lines. 5-bromo-2-(4-nitrobenzylidene) benzofuran-3(2H)-one demonstrated good antitumor activity against K562 cells with an IC50 of 0.37 lM. © Springer-Verlag Berlin Heidelberg 2014.