Synthesis, molecular docking and biological evaluation of quinolone derivatives as novel anticancer agents

Abstract

A series of novel quinolone derivatives (8a-j) were synthesized, and their anticancer activities were tested in human cancer cell lines, human lung carcinoma cell (A549), human promyelocytic leukemia cell (HL-60), and human cervical cancer cell (Hela). Compound 8i was found to be 5-times more potent in cellkilling activity for cell lines A549, HL-60, and Hela than the positive control irinotecan or cisplatin, with IC50 of 0.009, 0.008 and 0.010 μM, respectively. The docking study revealed that compound 8i might have strong interactions with the active site of DNA-topoisomerase I.