Synthesis of New 1,3,4-Oxadiazole-benzimidazole Derivatives as Potential Antioxidants and Breast Cancer Inhibitors with Apoptosis Inducing Activity

Abstract

Synthesis of new compounds combining benzimidazole with 1,3,4-oxadiazole functionalized by various alkyl and heterocyclic moieties is studied. The new hybrids were evaluated as DPPH radical scavengers and antioxidants. The most active compounds 1, 2, 3a, 3c, and 5d were tested as anticancer agents against MCF-7 and MDA-MB-231 breast cancer cells. The biological study demonstrated significant sensitivity of both types of cancer cells towards the synthesized compounds in comparison with erlotinib used as a reference drug. Cell cycle and apoptosis analysis indicated compound 5d as the one inducing G2/M phase arrest and apoptosis in MCF-7 and MDA-MB-231 cancer cells, in addition to its upregulation of caspases-3 and caspases-9.