Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR(L858R/T790M/C797S)
文献类型：期刊论文
| 作者 | Li, Qiannan1; Zhang, Tao2; Li, Shiliang1; Tong, Linjiang2; Li, Junyu1; Su, Zhicheng1; Feng, Fang2; Sun, Deheng1; Tong, Yi1; Wang, Xia1 |
| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2019-06-01 |
| 卷号 | 10期号:6页码:869-873 |
| 关键词 | EGFR mutant inhibitor C797S |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/acsmedchemlett.8b00564 |
| 通讯作者 | Li, Honglin(hlli@ecust.edu.cn) ; Xie, Hua(hxie@jding.dhs.org) ; Xu, Yufang(yfxu@ecust.edu.cn) |
| 英文摘要 | In this paper, we describe the discovery and optimization of a series of noncovalent reversible epidermal growth factor receptor inhibitors of EGFR(L858R/T790M/C797S). One of the most promising compounds, 25g, inhibited the enzymatic activity of EGFR(L8S8R/T790M/C797S) with an IC50 value of 2.2 nM. Cell proliferation assays showed that 25g effectively and selectively inhibited the growth of EGFR(L858R/T790M/C797S)-dependent cells. This series of compounds, which occupy both the ATP binding site and the allosteric site of the EGFR kinase, may serve as a basis for the development of fourth-generation EGFR inhibitors for L858R/T790M/C797S mutants. |
| WOS关键词 | CELL LUNG-CANCER ; ACQUIRED-RESISTANCE ; MUTATIONS ; GEFITINIB ; AZD9291 |
| 资助项目 | National Key Research and Development Program[2016YFA0502304] ; National Natural Science Foundation of China[81825020] ; National Natural Science Foundation of China[81803437] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002] ; Fundamental Research Funds for the Central Universities ; Special Program for Applied Research on Super Computation of the NSFC-Guangdong Joint Fund[U1501501] ; Shanghai Sailing Program[18YF1405100] ; National Program for Special Support of Eminent Professionals ; National Program for Support of Top-notch Young Professionals |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000471834600007 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/289363]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Li, Honglin; Xie, Hua; Xu, Yufang |
| 作者单位 | 1.East China Univ Sci & Technol, Sch Pharm, State Key Lab Bioreactor Engn, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Qiannan,Zhang, Tao,Li, Shiliang,et al. Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR(L858R/T790M/C797S)[J]. ACS MEDICINAL CHEMISTRY LETTERS,2019,10(6):869-873. |
| APA | Li, Qiannan.,Zhang, Tao.,Li, Shiliang.,Tong, Linjiang.,Li, Junyu.,...&Xu, Yufang.(2019).Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR(L858R/T790M/C797S).ACS MEDICINAL CHEMISTRY LETTERS,10(6),869-873. |
| MLA | Li, Qiannan,et al."Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR(L858R/T790M/C797S)".ACS MEDICINAL CHEMISTRY LETTERS 10.6(2019):869-873. |
入库方式： OAI收割
来源：上海药物研究所
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