Design, synthesis and apoptotic effects of novel benzoxazole compounds

Abstract

A series of new benzoxazole-hydrazone and benzoxazole-1,3,4-oxadiazole derivatives have been designed, synthesized and evaluated as cytotoxic agents toward human A549 lung cancer cells. Compounds 3d, 3e, 5b, 5c, 5d and 5e were the most potent compounds with IC₅₀ values of <3.9, 10.33, 11.6, 5.00, <3.9 and 4.5 μg/mL, respectively, which are higher than reference drug cisplatin (IC₅₀ = 19.00 μg/mL). The flow cytometry-based apoptosis detection assay was performed to determine their effects on apoptosis in A549 cells. All tested compounds induced apoptosis in A549 cell line.

Keywords: 1,3,4-oxadiazole; MTT; benzoxazole; hydrazone; lung cancer.