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. 国家新药筛选中心
Benzo[c][1,2,5] thiadiazole derivatives: A new class of potent Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors

文献类型：期刊论文

作者Wang, Wen-Long1,2; Chen, Xiao-Yu2; Gao, Ya2; Gao, Li-Xin1; Sheng, Li1; Zhu, Jingyu2; Xu, Lei3; Ding, Zhen-Zhong4; Zhang, Chao4; Li, Jing-Ya1
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2017-12-01
卷号27期号:23页码:5154-5157
关键词Benzo[c][1,2,5] thiadiazole derivatives PTP1B SHP2 Inhibitors Structure-activity relationships (SAR)
ISSN号0960-894X
DOI10.1016/j.bmcl.2017.10.059
文献子类Article
英文摘要The Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) is an oncogenic phosphatase linked to various kinds of cancers. Consequently, SHP2 has emerged as a promising target for novel anti-cancer agents. Using scaffold-hopping strategy, a series of benzo[c][1,2,5] thiadiazole derivatives was designed from PTP1B inhibitors with 1H-2,3-Dihydroperimidine motif, synthesized and evaluated their biological activities against PTP1B and SHP2. Among them, the representative compound 11g displayed SHP2 inhibitory activity with IC50 of 2.11 +/- 0.99 mu M, exhibited 2.02-fold and 25-fold selectivity for SHP2 over SHP1 and PTP1B respectively and had no visible activity against TCPTP. These preliminary results could provide a possible opportunity for the development of novel SHP2 inhibitors with optimal potency and improved pharmacological properties. (C) 2017 Elsevier Ltd. All rights reserved.
WOS关键词MOLECULE KINASE INHIBITORS ; CANCER ; 1B
资助项目National Natural Science Foundation of China[81125023] ; National Natural Science Foundation of China[21772068] ; State Key Laboratory of Drug Research[SIMM1705KF-01] ; Department of Science and Technology of Jiangsu Province[BY2016022-37]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000415643400013
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/272379]  
专题国家新药筛选中心
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Wang, Wen-Long; Zhou, Yu-Bo
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
2.Jiangnan Univ, Sch Pharmaceut Sci, Wuxi 214122, Peoples R China;
3.Jiangsu Univ Technol, Inst Bioinformat & Med Engn, Sch Elect & Informat Engn, Changzhou 213001, Peoples R China;
4.YangZhou RiXing Biotech Co Ltd, Yangzhou 225601, Jiangsu, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Wen-Long,Chen, Xiao-Yu,Gao, Ya,et al. Benzo[c][1,2,5] thiadiazole derivatives: A new class of potent Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2017,27(23):5154-5157.
APA Wang, Wen-Long.,Chen, Xiao-Yu.,Gao, Ya.,Gao, Li-Xin.,Sheng, Li.,...&Zhou, Yu-Bo.(2017).Benzo[c][1,2,5] thiadiazole derivatives: A new class of potent Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,27(23),5154-5157.
MLA Wang, Wen-Long,et al."Benzo[c][1,2,5] thiadiazole derivatives: A new class of potent Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27.23(2017):5154-5157.

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。