Novel benzofuran derivatives: Synthesis and antitumor activity

Abstract

A series of new benzofuran derivatives 3a-f, 5a-e containing a heterocyclic substituent linked to benzofuran nucleus at C-2 were synthesized as potential antitumor agents. These products were synthesized starting with 2-bromoacetylbenzofuran 1. The structures of all compounds were established on the basis of analytical and spectral data. The synthesized compounds were tested against human liver carcinoma cell line (HEPG2) and all were more potent than the comparative standard (5-flurouracil). Compound 3f was the most active (IC50 = 12.4μg/mL).