Abstract
A series of 2,5-diaryl-3-methylpyrimido[4,5-
c]quinolin-1(2
H)-ones (
7–
30), variously substituted at the 2- and 5-phenyl moieties, were synthesized and evaluated for their in vitro cytotoxic activity against a PC3 cancer cell line. Cytotoxicity data revealed that the type of substituent as well as substitution pattern have variable influence on cytotoxic activity. Among the compounds tested, compounds (
9), (
13), (
18), (
19), and (
23) demonstrated appreciable cytotoxic activity with mean IC
50 values of 2.0, 1.4, 1.6, 2.2, and 1.9
μM, respectively. Methyl substitution at the 2-phenyl ring was found to yield the least active compounds. Two of the most potent compounds (
13) and (
18) were further investigated for inhibition of tubulin polymerization and found to have no activity at the concentrations used in the assay.