Design, synthesis, and apoptotic antiproliferative action of new benzimidazole/1,2,3-triazole hybrids as EGFR inhibitors.

INTRODUCTION

This work outlines the design, synthesis, and biological evaluation of a new series of benzimidazole/1,2,3-triazole hybrids as apoptotic antiproliferative agents that inhibit the EGFR pathway.

METHODS

The research assesses the antiproliferative efficacy of compounds and against various cancer cell lines.

RESULTS AND DISCUSSION

The research emphasizing hybrids and for their remarkable activity, with GI values of 29 nM and 25 nM, respectively. The inhibitory effects of the most potent hybrids , , , , and on EGFR were assessed. Compounds and exhibited greater potency than erlotinib as EGFR inhibitors. Compounds and were also examined for their apoptotic potential, revealing that these compounds promote apoptosis by activating caspase-3, caspase-8, and Bax, while down-regulating the anti-apoptotic protein Bcl-2. Molecular docking experiments are thoroughly examined to validate the binding interactions of the most active hybrids, and , with the EGFR active site. Furthermore, our new study examined the ADME properties of the new hybrids.