Synthesis and evaluation of novel non-covalent binding quinazoline glycoside derivatives targeting the L858R and T790M variants of EGFR
文献类型：期刊论文
| 作者 | Zhang, Renshuai1; Chen, Shaopeng1; Zhang, Xiaowei2; Yu, Rilei1; Wan, Shengbiao1; Geng, Meiyu2 ; Jiang, Tao1
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| 刊名 | RSC ADVANCES
 |
| 出版日期 | 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. |
| WOS关键词 | CELL LUNG-CANCER ; TYROSINE KINASE ; INHIBITOR ; RECEPTOR ; RESISTANCE ; THERAPY |
| 资助项目 | Natural Science Foundation of China[81373322] ; Natural Science Foundation of China[21171154] ; CMST[2013DFG32160] ; NSFC[U1406402] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000374561300076 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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