ANTITUMOR ACTIVITY OF IMIDAZO [4, 5-g] QUINOLINE DERIVATIVES

Abstract

Fifty imidazo [4, 5-g] quinoline derivatives were synthesized and their antitumor activities were tested against Ehrlich ascites carcinoma, and mouse leukemias L-1210 and P388. These derivatives were administered intraperitoneally in the form of suspension. 1, 3-Dimethyl-1, 2, 5, 8-tetrahydro-2, 8-dioxoimidazo [4, 5-g] quinoline-7-carbohydroxamates with relatively small alkyl groups, ethyl (24), 2-butenyl (44), butyl (33) and vinyl (41) moiety, at the 5 position, were found to be highly effective against Ehrlich carcinoma (30-day survival≨67%). Three derivatives, compounds 41 and 44, and 1, 3-dimethyl-5-vinyl-1, 2, 5, 8-tetrahydro-2, 8-dioxoimidazo [4, 5-g] quinoline-7-carboxylic acid (15), increased the lifespan of mice bearing leukemia L-1210 to more than 50% over the control. Compounds 41 and 44 were also found to be active against mouse leukemia P388.