中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
  4. 新药研究国家重点实验室
Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation

文献类型：期刊论文

作者Xu, Dandan1,3; Sun, Deqiao2,3,4; Wang, Wei1,3; Peng, Xia2; Zhan, Zhengsheng1; Ji, Yinchun2; Shen, Yanyan2; Geng, Meiyu2,3,4; Ai, Jing2,3,5; Duan, Wenhu1,3
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2021-08-05
卷号220页码:18
关键词Axl Cancer Inhibitor Pyrrolo[2,3-d]pyrimidine
ISSN号0223-5234
DOI10.1016/j.ejmech.2021.113497
通讯作者Ai, Jing(jai@simm.ac.cn) ; Duan, Wenhu(whduan@simm.ac.cn)
英文摘要Axl has emerged as an attractive target for cancer therapy due to its strong correlation with tumor growth, metastasis, poor survival, and drug resistance. Herein, we report the design, synthesis and structure-activity relationship (SAR) investigation of a series of pyrrolo[2,3-d]pyrimidine derivatives as new Axl inhibitors. Among them, the most promising compound 13b showed high enzymatic and cellular Axl potencies. Furthermore, 13b possessed preferable pharmacokinetic properties and displayed promising therapeutic effect in BaF3/TEL-Axl xenograft tumor model. Compound 13b may serve as a lead compound for new antitumor drug discovery. (C) 2021 Elsevier Masson SAS. All rights reserved.
WOS关键词RECEPTOR TYROSINE KINASE ; TO-MESENCHYMAL TRANSITION ; SMALL-MOLECULE INHIBITOR ; CELL LUNG-CANCER ; C-MET ; THERAPEUTIC TARGET ; PHASE-I ; ANTITUMOR EFFICACY ; DRUG-RESISTANCE ; TAM RECEPTORS
资助项目National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002-011-016] ; Science and Technology Commission of Shanghai Municipality[18431907100] ; National Natural Science Foundation of China[21702220] ; National Natural Science Foundation of China[81773762] ; Youth Innovation Promotion Association CAS[2018324] ; Personalized Medicines -Molecular Signature-based Drug Discovery and Development Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020000] ; Personalized Medicines -Molecular Signature-based Drug Discovery and Development Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020103] ; Collaborative Innovation Cluster Project of Shanghai Municipal Commission of Health and Family Planning[2020CXJQ02]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000659148800036
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/296964]  
专题新药研究国家重点实验室
通讯作者Ai, Jing; Duan, Wenhu
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China
3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
4.Shanghai Tech Univ, Sch Life Sci & Technol, 393 Middle Huaxia Rd, Shanghai 201210, Peoples R China
5.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, 1 Xiangshan Branch Lane, Hangzhou 330106, Peoples R China
推荐引用方式
GB/T 7714		 Xu, Dandan,Sun, Deqiao,Wang, Wei,et al. Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2021,220:18.
APA Xu, Dandan.,Sun, Deqiao.,Wang, Wei.,Peng, Xia.,Zhan, Zhengsheng.,...&Duan, Wenhu.(2021).Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,220,18.
MLA Xu, Dandan,et al."Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 220(2021):18.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。