國家衛生研究院 NHRI:Item 3990099045/3977

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Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/3977

Title:	Identification, SAR studies, and X-ray Co-crystallographic analysis of a novel furanopyrimidine aurora kinase a inhibitor
Authors:	Coumar, MS;Tsai, MT;Chu, CY;Uang, BJ;Lin, WH;Chang, CY;Chang, TY;Leou, JS;Teng, CH;Wu, JS;Fang, MY;Chen, CH;Hsu, JTA;Wu, SY;Chao, YS;Hsieh, HP
Contributors:	Division of Biotechnology and Pharmaceutical Research
Abstract:	Herein we reveal a simple method for the identification of novel Aurora kinase A inhibitors through substructure searching of an in-house compound library to select compounds for testing. A hydrazone fragment conferring Aurora kinase activity and heterocyclic rings most frequently reported in kinase inhibitors were used as substructure queries to filter the in-house compound library collection prior to testing. Five new series of Aurora kinase inhibitors were identified through this strategy, with IC<sub>50</sub> values ranging from ? 300 nm to ? 15 μm, by testing only 133 compounds from a database of ? 125 000 compounds. Structure-activity relationship studies and X-ray co-crystallographic analysis of the most potent compound, a furanopyrimidine derivative with an IC<sub>50</sub> value of 309 nm toward Aurora kinase A, were carried out. The knowledge gained through these studies could help in the future design of potent Aurora kinase inhibitors.
Date:	2010-02-01
Relation:	ChemMedChem. 2010 Feb 1;5(2):255-267.
Link to:	http://dx.doi.org/10.1002/cmdc.200900339
JIF/Ranking 2023:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1860-7179&DestApp=IC2JCR
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000274538600010
Cited Times(Scopus):	http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=75749152578
Appears in Collections:	[Hsing-Pang Hsieh] Periodical Articles [Su-Ying Wu] Periodical Articles [John Tsu-An Hsu] Periodical Articles [Yu-Sheng Chao(2002-2013)] Periodical Articles

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