Synthesis and Cytotoxicity of 2-Phenylquinazolin-4-thiones

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Title:	Synthesis and Cytotoxicity of 2-Phenylquinazolin-4-thiones
Authors:	連金城(Lien,Jin-Cherng);侯曼貞(Hour,Mann-Jen);黃麗嬌(Huang,Li-Jiau);郭盛助(Kuo,Sheng-Chu)
Contributors:	藥學院藥物化學研究所
Date:	2004-03-05
Issue Date:	2009-09-07 12:11:25 (UTC+8)
Abstract:	Synthesis and Cytotoxicity of 2-Phenylquinazolin-4-thiones Jin-Cherng Lien1（連金城）, Mann-Jen Hour2（侯曼貞）, Li-Jiau Huang1（黃麗嬌）, and Sheng-Chu Kuo1（郭盛助） 1Graduate Institute of Pharmaceutical Chemistry, China Medical University, Taichung, Taiwan 2School of Pharmacy, China Medical University, Taichung, Taiwan In our continuing search for potential anticancer candidates, a series of 6,7,2',3',4',5'-substituted 2-phenylquinazolin-4-ones has been synthesized and evaluated for their cytotoxicity and as inhibitors of tubulin polymerization. In general, a good correlation was found between the two kinds of activity. Therefore, we are intending to synthesize a series of analogs, 2-phenylquinazolin-4-thiones. First, 5-substituted anthranilamide and bezaldehyde (or 3-methoxybenzaldehyde) were condensed in the presence of sodium bisulfite to afford 6- and 3’-substituted 2-phenylquinazolin-4-ones, and then, they are reacted with P2S5 to obtain target compounds. And now these compounds have been submitted for evaluating their cytotoxicity and ITP (inhibition of tubulin polymerization). Hopefully, the structure-activity relationship of these heterocyclic ketones and potential new leads would be established.
Relation:	2004藥物化學研討會
Appears in Collections:	[Graduate Institute of Pharmaceutical Chemistry] Proceedings

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