Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors

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Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors

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作者：Long Zhang ; Yingying Yang ; Haojie Zhou ; Qingmei Zheng ; Yuhao Li ; Shansong Zheng ; Shuyong Zhao ; Dong Chen ; Chuanwen Fan ; ^{chuanwen.fan@qilu-pharma.com" class="auth_mail" title="E-mail the corresponding author}
关键词：Quinazoline derivatives ; H1975 ; EGFR-T790M ; HCC827 ; A-431
刊名：European Journal of Medicinal Chemistry
出版年：2015
出版时间：18 September 2015
年：2015
卷：102
期：Complete
页码：445-463
全文大小：6833 K

文摘

class="label">•: Structure-activity relationship of quinazoline derivatives was described.
class="label">•: New compounds showed massive improvements over afatinib against H1975.
class="label">•: Two safe and effective irreversible inhibitors (class="boldFont">7q & class="boldFont">8f) were discovered.
class="label">•: class="boldFont">7q and class="boldFont">8f showed higher in vivo efficacy and safety than afatinib against H1975.
class="label">•: class="boldFont">7q and class="boldFont">8f demonstrated good pharmacokinetic profiles and oral bioavailability.

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