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Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis and biological activity of 2,5-diaryl-3-methylpyrimido[4,5-c]quinolin-1(2H)-one derivatives
Kamel Metwally1, Omar Aly, Enayat Aly
1Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. kametwally@hotmail.com
Abstract:
A series of 2,5-diaryl-3-methylpyrimido[4,5-c]quinolin-1(2H)-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 1.9microM, 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.
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