Synthesis and biological evaluation of heterocyclic bis-aryl amides as novel Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors
文献类型：期刊论文
| 作者 | Satheeshkumar, Rajendran1; Zhu, Rui1; Feng, Bo1; Huang, Chao1; Gao, Ya1; Gao, Li-Xin2; Shen, Chao3; Hou, Ting-Jun3; Xu, Lei4; Li, Jia2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2020-06-01 |
| 卷号 | 30期号:11页码:5 |
| ISSN号 | 0960-894X |
| 关键词 | Heterocyclic bis-aryl amides PTP1B SHP2 Inhibitors Structure-activity relationships (SAR) |
| DOI | 10.1016/j.bmcl.2020.127170 |
| 通讯作者 | Zhu, Yun-Long(sequoia113847@163.com) ; Zhou, Yu-Bo(ybzhou@simm.ac.cn) ; Wang, Wen-Long(wwenlong2011@163.com) |
| 英文摘要 | The Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) is a convergent node for oncogenic cell-signaling cascades including the PD-L1/PD-1 pathway. Consequently, SHP2 has emerged as a compelling target for novel anti-cancer agents. Replacing one of phenyl ring in PTP1B inhibitor 1 with heterocyclic ring led to a series of heterocyclic bis-aryl amide derivatives. The representative compound 7b displayed SHP2 inhibitory activity with IC50 of 2.63 +/- 0.08 mu M, exhibited about 4-fold selectivity for SHP2 over TCPTP and had no detectable activity against SHP1 and PTP1B. These preliminary results could provide a possible opportunity for the development of novel SHP2 inhibitors with optimal potency and improved pharmacological properties. |
| WOS关键词 | ALLOSTERIC INHIBITION ; DERIVATIVES ; PTP1B |
| 资助项目 | National Natural Science Foundation of China[21772068] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002] ; Natural Science Foundation of Jiangsu Province[BK20190608] ; Jiangsu Province Postdoctoral Science Foundation[2019K220] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| WOS记录号 | WOS:000526087400023 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/281049]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhu, Yun-Long; Zhou, Yu-Bo; Wang, Wen-Long |
| 作者单位 | 1.Jiangnan Univ, Sch Pharmaceut Sci, Wuxi 214122, Jiangsu, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou Inst Innovat Med, Hangzhou 310058, Peoples R China 4.Jiangsu Univ Technol, Sch Elect & Informat Engn, Inst Bioinformat & Med Engn, Changzhou 213001, Peoples R China 5.Nanjing Med Univ, Affiliated Wuxi Matern & Child Hlth Care Hosp, Wuxi 214002, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Satheeshkumar, Rajendran,Zhu, Rui,Feng, Bo,et al. Synthesis and biological evaluation of heterocyclic bis-aryl amides as novel Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2020,30(11):5. |
| APA | Satheeshkumar, Rajendran.,Zhu, Rui.,Feng, Bo.,Huang, Chao.,Gao, Ya.,...&Wang, Wen-Long.(2020).Synthesis and biological evaluation of heterocyclic bis-aryl amides as novel Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,30(11),5. |
| MLA | Satheeshkumar, Rajendran,et al."Synthesis and biological evaluation of heterocyclic bis-aryl amides as novel Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 30.11(2020):5. |
入库方式： OAI收割
来源：上海药物研究所
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