Mercuric chloride catalyzed synthesis of some anticancer 2-aryl-2,3-dihydroquinizolin-4(1H)-ones

Abstract

A series of ten 2,3-dihydroquinizolin-4(1H)-one derivatives were synthesized by ethanol-mediated condensation of anthranilamide with various aryl aldehydes in presence of catalytic amount of mercuric chloride (HgCl2). The temperature of the reactions was maintained at 60 °C for good yield of the products. The highlights of the method include use of lab grade of chemicals as reagents and ease of work up in obtaining the product with high purity. Out of ten derivatives synthesized, three compounds 3f, 3i, and 3j are new and all the compounds were evaluated for their cytotoxic activity against six cancer cell lines. The compounds 3b (IC50: 26.1 µg mL−1), 3c (42.7 µg mL−1) ,and 3e (31.1 µg mL−1) have shown activity against the cell line MDA-MB-231. Compounds 3b, 3c, 3d, 3e, and 3g showed significant total growth inhibition (TGI) values against the cell line MDA-MB-231 and compound 3j showed good TGI value against the cell line PANC 1. Compounds were also screened for their antibacterial activity and antioxidant activity by DPPH method.