Design and Synthesis of Unsymmetric Benzils, Quinoxalines, and Evaluations of their Anticancer Activities against Human Non-Small Lung Cancer Cells

ChemMedChem. 2024 Nov 26:e202400847. doi: 10.1002/cmdc.202400847. Online ahead of print.

Abstract

Quinoxaline and its derivatives exhibit a broad spectrum of biological activity, making them valuable for various therapeutic applications. However, most quinoxalines are synthetically produced due to their scarcity in nature. In this article, a series of unsymmetric benzils were synthesized and subsequently condensed with 1,2-diaminobenzene to produce unsymmetric quinoxalines. The novel synthetic benzils and quinoxalines were evaluated for their anticancer activities against human non-small-cell lung cancer (NSCLC) cells harboring different gene mutations, to explore their potential as anticancer agents. Among these synthesized molecules, compound 5 g demonstrated inhibitory effects comparable to those of cisplatin.

Keywords: Anticancer activities; Sonogarshira reaction; Unsymmetric benzil; Unsymmetric quinoxaline.