Synthesis and evaluation of novel non-covalent binding quinazoline glycoside derivatives targeting the L858R and T790M variants of EGFR

doi:10.1039/c6ra06818a

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	Synthesis and evaluation of novel non-covalent binding quinazoline glycoside derivatives targeting the L858R and T790M variants of EGFR
	Zhang, Renshuai 1; Chen, Shaopeng 1; Zhang, Xiaowei 2; Yu, Rilei 1; Wan, Shengbiao 1; Geng, Meiyu2 ; Jiang, Tao 1
刊名	RSC ADVANCES
	2016
卷号	6 期号:43 页码:36857-36862
ISSN号	2046-2069
DOI	10.1039/c6ra06818a
文献子类	Article
英文摘要	A series of novel quinazoline glycoside derivatives were designed, synthesized, and evaluated for their inhibition activities against EGFRWT, EGFR/L858R/T790M, and skin epidermoid carcinoma cell line (A431). Several L-rhamnose derivatives were found to be as efficient as the irreversible inhibitor HKI-272 or BIBW2992 in inhibiting EGFR/T790M/L858R. Molecular dynamic simulations indicated that the saccharide group plays a significant role in stabilization of the quinazoline glycoside derivative through the hydrogen bonding with several polar residues at the edge of the ATP-binding cleft.
资助项目	Natural Science Foundation of China[81373322] ; Natural Science Foundation of China[21171154] ; CMST[2013DFG32160] ; NSFC[U1406402]
WOS关键词	CELL LUNG-CANCER ; TYROSINE KINASE ; INHIBITOR ; RECEPTOR ; RESISTANCE ; THERAPY
WOS研究方向	Chemistry
语种	英语
出版者	ROYAL SOC CHEMISTRY
WOS记录号	WOS:000374561300076
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276232]
专题	药理学第一研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Geng, Meiyu; Jiang, Tao
作者单位	1.Ocean Univ China, Sch Med & Pharm, Key Lab Marine Drugs, Minist Educ China, Qingdao 266003, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Renshuai,Chen, Shaopeng,Zhang, Xiaowei,et al. Synthesis and evaluation of novel non-covalent binding quinazoline glycoside derivatives targeting the L858R and T790M variants of EGFR[J]. RSC ADVANCES,2016,6(43):36857-36862.
APA	Zhang, Renshuai.,Chen, Shaopeng.,Zhang, Xiaowei.,Yu, Rilei.,Wan, Shengbiao.,...&Jiang, Tao.(2016).Synthesis and evaluation of novel non-covalent binding quinazoline glycoside derivatives targeting the L858R and T790M variants of EGFR.RSC ADVANCES,6(43),36857-36862.
MLA	Zhang, Renshuai,et al."Synthesis and evaluation of novel non-covalent binding quinazoline glycoside derivatives targeting the L858R and T790M variants of EGFR".RSC ADVANCES 6.43(2016):36857-36862.