Synthesis, molecular modeling and biological evaluation of 2-aminomethyl-5-(quinolin-2-yl)-1,3,4-oxadiazole-2(3H)-thione quinolone derivatives as novel anticancer agent

A series of quinoline derivatives (4a–4o) have been synthesized and their biological activities were also evaluated as potential telomerase inhibitors. Bioassay tests demonstrated that most of the compounds exhibited substantial broad-spectrum antitumor activity against the three cancer cell lines (HepG2, SGC-7901 and MCF-7). Moreover, all the title compounds were assayed for telomerase inhibition using the TRAP-PCR-ELISA assay. Compounds 4d and 4i displayed the most potent anticancer activities, which were comparable to the positive control. Docking simulation was performed to position compounds 4d and 4i into the telomerase structure active site to determine the probable binding model. Compounds 4d and 4i with potent inhibitory activity in tumor growth inhibition may be potential anticancer agents.

New quinoline derivatives have been designed and evaluated for their telomerase inhibitory activity and anticancer activity. The most active compounds are 4d and 4i.Figure optionsDownload as PowerPoint slideHighlights
► The synthesis and anticancer activities of these compounds have not been reported so far.
► Our current findings are completely new.
► Their biological activities are also evaluated for telomerase inhibitory activity.