國家衛生研究院 NHRI:Item 3990099045/5206

NHRI > Institute of Biotechnology and Pharmaceutical Research > Yu-Sheng Chao(2002-2013) > Periodical Articles > Item 3990099045/5206

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/5206

Title:	Design and synthesis of tetrahydropyridothieno[2,3-d]pyrimidine scaffold based epidermal growth factor receptor (EGFR) kinase inhibitors: the role of side chain chirality and michael acceptor group for maximal potency
Authors:	Wu, CH;Coumar, MS;Chu, CY;Lin, WH;Chen, YR;Chen, CT;Shiao, HY;Rafi, S;Wang, SY;Hsu, H;Chen, CH;Chang, CY;Chang, TY;Lien, TW;Fang, MY;Yeh, KC;Chen, CP;Yeh, TK;Hsieh, SH;Hsu, JT;Liao, CC;Chao, YS;Hsieh, HP
Contributors:	Institute of Biotechnology and Pharmaceutical Research;Division of Molecular and Genomic Medicine
Abstract:	HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 antiproliferative activity compared to HTS hit 7 and also inhibited gefitinib-resistant double mutant (DM, T790M/L858R) EGFR kinase at nanomolar concentration. Moreover, treatment with 19 shrinked tumor in nude mice xenograft model.
Date:	2010-10-28
Relation:	Journal of Medicinal Chemistry. 2010 Oct 28;53(20):7316-7326.
Link to:	http://dx.doi.org/10.1021/jm100607r
JIF/Ranking 2023:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000283106300005
Cited Times(Scopus):	http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77958465100
Appears in Collections:	[趙宇生(2002-2013)] 期刊論文 [陳炯東] 期刊論文 [葉燈光] 期刊論文 [徐祖安] 期刊論文 [謝興邦] 期刊論文 [陳怡榮] 期刊論文

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