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Synthesis and biological activity of 2,5-diaryl-3methylpyrimido{[}4,5-c]quinolin-1(2H)-one derivatives
Faculty
Pharmacy
Year:
2007
Type of Publication:
Article
Pages:
2434-2440
Authors:
Metwally, Kamel, Aly, Omar, Aly, Enayat, Banerjee, Abhijit, Ravindra, Rudravajhala, Bane, Susan
DOI:
10.1016/j.bmc.2007.01.016
Journal:
BIOORGANIC \& MEDICINAL CHEMISTRY PERGAMON-ELSEVIER SCIENCE LTD
Volume:
15
Research Area:
Biochemistry \& Molecular Biology; Pharmacology \& Pharmacy; Chemistry
ISSN
ISI:000244774100017
Keywords :
cytotoxic agents, tubulin polymerization, pyrimido[4, 5-c], quinolin-1(2H)-ones
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 IC50 values of 2.0, 1.4, 1.6, 2.2, and 1.9 mu M, 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. (c) 2007 Elsevier Ltd. All rights reserved.
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