Design, synthesis and evaluation of cytotoxicity of novel chromeno[4,3-b]quinoline derivatives

Abstract

In the present work 15 new 1,4-dihydropyridines (DHPs) bearing a coumarin ring were synthesized and assessed on 4 different human cancer cell lines (HeLa, K562, LS180, and MCF-7). Although, all the derivatives were inactive on LS180 cell line, the results on other cells showed that these compounds had weak to moderate antitumoral activities and their IC(50) ranged from 25 to >100 µM. Among the synthesized compounds, 7-(2-nitrophenyl)-8,9,10,12-tetrahydro-7H-chromeno[4,3-b]quinoline-6,8-dione (6a) demonstrated the highest activity (IC(50) range in different cell lines: 25.4-58.6 µM). Furthermore, the calcium channel antagonist activity of the derivatives, an undesired effect when these compounds are used as antitumoral agents, was much lower than nifedipine, a reference antagonist. In conclusion, this group of compounds seems to have promising biological properties and further investigation on this group could potentially lead to the discovery of cytotoxic agents with low calcium channel blocking activity.