國家衛生研究院 NHRI:Item 3990099045/7571

NHRI > Institute of Biotechnology and Pharmaceutical Research > Hsing-Pang Hsieh > Conference Papers/Meeting Abstract > Item 3990099045/7571

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/7571

Title:	Design and synthesis of Aurora kinase inhibitors as anticancer agents
Authors:	Hsu, YC;Shiao, HY;Lin, WH;Hsu, JTA;Chen, CT;Chao, YS;Hsieh, HP
Contributors:	Institute of Biotechnology and Pharmaceutical Research
Abstract:	In our preliminary result, compound 1 , which contained the urea side chain and di-substituted furanopyrimidine core structure, possessed Aurora A kinase inhibition with an IC50 of 43 nM and anti-proliferation against HCT-116 with an IC50 of 400 nM. In the present work, we applied the scaffold-hopping strategy to explore the structure-activity relationship of this series of kinase inhibitors. Based on the bioisosterism, various five-member heterocyclic-fused pyrimidine cores with a variety of substitutents were synthesized to replace the furanopyrimidine moiety, such as thiopheno-, oxazolo-, imidazolo-, pyrrolo-pyrimidine and quinazoline. It is noted that the inhibitors containing thienopyrimidine or quinazoline as core structure revealed the remarkable antiproliferative activity with the low IC50 value of 21 nM and 20 nM, respectively. After introducing the solubilizing group into quinazoline core, the final compound showed significant in vivo antiproliferative activity in HCT-116 tumor xenograft model.
Date:	2013-04
Relation:	Abstracts of Papers - American Chemical Society. 2013 Apr;245:Article number 301-MEDI.
Link to:	http://abstracts.acs.org/chem/245nm/program/view.php?pub_num=301&par=MEDI
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000324303602321
Appears in Collections:	[Hsing-Pang Hsieh] Conference Papers/Meeting Abstract [John Tsu-An Hsu] Conference Papers/Meeting Abstract [Yu-Sheng Chao(2002-2013)] Conference Papers/Meeting Abstract [Chiung-Tong Chen] Conference Papers/Meeting Abstract

Files in This Item:

File	Description	Size	Format
ISI000324303602321.pdf		313Kb	Adobe PDF	560	View/Open

Loading...