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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

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dc.citation.epage7326en_US
dc.citation.issue20en_US
dc.citation.spage7316en_US
dc.citation.volume53en_US
dc.contributor.authorWu, Chia-Hsienen_US
dc.contributor.authorCoumar, Mohane Selvarajen_US
dc.contributor.authorChu, Chang-Yingen_US
dc.contributor.authorLin, Wen-Hsingen_US
dc.contributor.authorChen, Yi-Rongen_US
dc.contributor.authorChen, Chiung-Tongen_US
dc.contributor.authorShiao, Hui-Yien_US
dc.contributor.authorRafi, Shaiken_US
dc.contributor.authorWang, Sing-Yien_US
dc.contributor.authorHsu, Huien_US
dc.contributor.authorChen, Chun-Hwaen_US
dc.contributor.authorChang, Chun-Yuen_US
dc.contributor.authorChang, Teng-Yuanen_US
dc.contributor.authorLien, Tzu-Wenen_US
dc.contributor.authorFang, Ming-Yuen_US
dc.contributor.authorYeh, Kai-Chiaen_US
dc.contributor.authorChen, Ching-Pingen_US
dc.contributor.authorYeh, Teng-Kuangen_US
dc.contributor.authorHsieh, Su-Hueien_US
dc.contributor.authorHsu, John T. -A.en_US
dc.contributor.authorLiao, Chun-Chenen_US
dc.contributor.authorChao, Yu-Shengen_US
dc.contributor.authorHsieh, Hsing-Pangen_US
dc.contributor.department生物科技學系zh_TW
dc.contributor.departmentDepartment of Biological Science and Technologyen_US
dc.date.accessioned2014-12-08T15:48:04Z
dc.date.available2014-12-08T15:48:04Z
dc.date.issued2010-10-28en_US
dc.description.abstractHTS 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.en_US
dc.identifier.doi10.1021/jm100607ren_US
dc.identifier.issn0022-2623en_US
dc.identifier.journalJOURNAL OF MEDICINAL CHEMISTRYen_US
dc.identifier.urihttp://dx.doi.org/10.1021/jm100607ren_US
dc.identifier.urihttps://ir.lib.nycu.edu.tw/handle/11536/32051
dc.language.isoen_USen_US
dc.titleDesign 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 Potencyen_US
dc.typeArticleen_US

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