國家衛生研究院 NHRI:Item 3990099045/6249

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Title:	Lead optimization of furanopyrimidine Aurora kinase inhibitors: Development of in vivo active agents in tumor xenograft models
Authors:	Hsieh, HP;Chu, CY;Coumar, MS;Lin, WH;Chen, CT;Hsu, TA;Wu, SY;Chao, YS
Contributors:	Institute of Biotechnology and Pharmaceutical Research
Abstract:	We have recently identified BPR1K432 (1), 1 a potent Aurora kinase A inhibitor (IC 50 ~50 nM), which possessed anti-proliferative activity in HCT-116 cell line (IC 50 ~400 nM). However, it was inactive in HCT-116 tumor xenograft nude mouse model. Hence we initiated optimization of the lead 1. Structure-activity relationship studies in the urea side chain (Strategy II) and modification in the phenyl rings (Strategy I) were carried out, resulting in the identification of BPR1K724, with improved drug like property and better in vitro anti-proliferative activity than the lead 1. Most importantly, the optimized lead BPR1K724 showed potent in vivo anti-tumor efficacy in HCT-116 tumor xenograft nude mouse model. The detailed SAR study leading to the identification of optimized lead BPR1K724 will be disclosed.
Date:	2010-08
Relation:	Abstracts of Papers - American Chemical Society. 2010 Aug;240:MEDI 332.
Link to:	http://www.acsmedchem.org/mediabstractf2010.pdf
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000208164704233
Appears in Collections:	[Hsing-Pang Hsieh] Conference Papers/Meeting Abstract [Su-Ying Wu] Conference Papers/Meeting Abstract [John Tsu-An Hsu] Conference Papers/Meeting Abstract [Chiung-Tong Chen] Conference Papers/Meeting Abstract [Yu-Sheng Chao(2002-2013)] Conference Papers/Meeting Abstract

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