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Pyrimido {[}4,5-c]quinolin-1(2H)-ones as a novel class of antimitotic agents: Synthesis and in vitro cytotoxic activity
Faculty
Pharmacy
Year:
2007
Type of Publication:
Article
Pages:
344-350
Authors:
Metwally, Kamel, Pratsinis, Harris, Kletsas, Dimitris
DOI:
10.1016/j.ejmech.2006.10.008
Journal:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Volume:
42
Research Area:
Pharmacology \& Pharmacy
ISSN
ISI:000245475900006
Keywords :
cytotoxic agents, antimitotic, pyrimido [4, 5-c]quinolin, 1(2H)-ones
Abstract:
Several 2-amino-pyrimido {[}4,5-c] quinolin-1(2H)-ones variously substituted at positions 3, 5, and 9 were prepared from their corresponding lactones. The target compounds were investigated for in vitro cytotoxic activity against a panel of human cancer cell lines, namely, lung fibrosarcoma HT-1080, colon adenocarcinoma HT-29, and breast carcinoma MDA-MB-231. Analysis of data revealed that the presence of chloro at position 9 has a major positive impact on cytotoxic activity. Additional halogen substitution at the para position of the 3-phenyl group further enhances activity. Furthermore, compound (25) was found to dose-dependently inhibit tubulin polymerization. In accordance, flow cytometric analysis of the most potent compounds (23-26) indicated that the tested compounds induce cell cycle arrest in the G(2)/M phase. The obtained results introduce the rarely described pyrimido {[}4,5-c]quinolin-1(2H)-one ring system as a new scaffold for promising antimitotic agents. (c) 2006 Elsevier Masson SAS. All rights reserved.
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