國家衛生研究院 NHRI:Item 3990099045/8104

NHRI > Institute of Biotechnology and Pharmaceutical Research > Shau-Hua Ueng > Periodical Articles > Item 3990099045/8104

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/8104

Title:	Discovery and structure-activity relationships of phenyl benzenesulfonylhydrazides as novel indoleamine 2,3-dioxygenase inhibitors
Authors:	Cheng, MF;Hung, MS;Song, JS;Lin, SY;Liao, FY;Wu, MH;Hsiao, W;Hsieh, CL;Wu, JS;Chao, YS;Shih, C;Wu, SY;Ueng, SH
Contributors:	Institute of Biotechnology and Pharmaceutical Research
Abstract:	A novel class of phenyl benzenesulfonylhydrazides has been identified as potent inhibitors of indoleamine 2,3-dioxygenase (IDO), and their structure-activity relationship was explored. Coupling reactions between various benzenesulfonyl chlorides and phenylhydrazides were utilized to synthesize the sulfonylhydrazides bearing various substituents. Compound 3i exhibited 61 nM of IC50 in enzymatic assay and 172 nM of EC50 in the HeLa cell. The computational study of 3i suggested that the major interactions between 3i and IDO protein are the coordination of sulfone and heme iron, the hydrogen bonding and hydrophobic interactions between 3i and IDO. This novel class of IDO inhibitor provides a new direction to discover effective anti-cancer agents.
Date:	2014-08
Relation:	Bioorganic and Medicinal Chemistry Letters. 2014 Aug;24(15):3403-3406.
Link to:	http://dx.doi.org/10.1016/j.bmcl.2014.05.084
JIF/Ranking 2023:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0960-894X&DestApp=IC2JCR
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000339228700037
Cited Times(Scopus):	http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84904059888
Appears in Collections:	[Shau-Hua Ueng] Periodical Articles [Su-Ying Wu] Periodical Articles [Yu-Sheng Chao(2002-2013)] Periodical Articles [Ming-Shiu Hung] Periodical Articles [Chuan Shih(2014-2017)] Periodical Articles [Shu-Yu Lin] Periodical Articles

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