Synthesis of acridine cyclic imide hybrid molecules and their evaluation for anticancer activity

Abstract

9-Amino acridine derivatives (1a-e) on condensation with dihydrofuran-2,5-dione, hexahydroisobenzofuran-1,3-dione and isochroman-1,3-dione under microwave irradiation gave corresponding condensation products 2a-e, 3a-e and 4a-e, respectively, in good yields. All these compounds were screened in vitro for anticancer activity against five human cancer cell lines, i.e., breast (T47D), lung (NCl H-522), colon (HCT-15), ovary (PA-1) and liver (Hep G2). Compounds 1-(3-methoxyacridine-9-yl) pyrrolidine-2,5-dione (2d) (ovary PA-1), 2-(2-methylacridine-9-yl)hexahydro-1H-isoindole-1,3(2H)-dione (3b) (lung NCl H-522), 2-(4-methylacridine-9-yl)hexahydro-1H-isoindole-1,3(2H)-dione (3c) (ovary PA-1), 2-(4-methoxyacridine-9-yl)hexahydro-1H-isoindole-1,3(2H)-dione (3e) (ovary PA-1) and 2-(2-methylacridine-9-yl)isoquinoline-1,3(2H,4H)-dione (4b) (ovary PA-1) exhibited IC<inf>50</inf> values 7.1, 8.0, 5.4, 10.0 and 6.56 ?M, respectively, and hence possess good anticancer activity. © 2015 Springer Science+Business Media New York.