Synthesis and anticancer activity of novel tetrahydroquinoline and tetrahydropyrimidoquinoline derivatives

Abstract

A series of new tetrahydroquinolines with different substituents at C-2 and C-4 positions in addition to several tetrahydropyrimidoquinolin-4-amines and tetrahydropyrimidoquinoline-2,4-diamines were synthesized. The in vitro anticancer activity of all newly synthesized compounds was tested against human colon carcinoma (HCT116) and human breast adenocarcinoma (MCF7) cell lines. Seven compounds 1a, 5a, 5b, 6a, 6b, 7a and 7b showed potent anticancer activity against both HCT116 and MCF7 cell lines with IC50 between 16.33 and 34.28 µM. All these compounds were more potent than imatinib (IC50 = 34.40 µM) and tamoxifen (IC50 = 34.30 µM). Compound 7b was the most active against HCT116 cell line with 2.1-fold more potent antitumor activity than imatinib. Also, compounds 1a, 5b and 6a exhibited the highest anticancer activity against MCF7 cell line, having two- to 1.79-fold more potent anticancer activity than tamoxifen.