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Anticancer activity of imidazole fused quinoxalines via human topoisomerase inhibition
Author : Gaurav Joshi and Raj Kumar*
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ABSTRACT
We herein report design, synthesis of imidazo[1,2-a]quinoxaline (4A-4E) via acid-catalyzed Pictet-Spengler (PS) reaction, and their anticancer assessment through inhibition of human topoisomerases. Two compounds 4D and 4E were found to be dual inhibitors of human topoisomerases and possessed anticancer potential at the low micromolar concentration (IC50 < 4.5 μM) in A549 (lung cancer), HT-29 (colon cancer) and MDA-MB-231 (breast cancer) cells. The molecules were also able to alter the intracellular ROS levels inside cancer cells and led to apoptosis via the mitochondrial independent pathway.
KEYWORD
Anticancer, imidazo[1,2-a]quinoxalines, topoisomerases, Pictet-Spengler reaction, molecular modeling