Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors
文献类型：期刊论文
| 作者 | Yang, Bowen1,3; Wu, Qian2; Huan, Xiajuan2; Wang, Yingqing2 ; Sun, Yin3; Yang, Yueyue1; Liu, Tongchao1; Wang, Xin1; Chen, Lin1; Xiong, Bing1
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2021-02-01 |
| 卷号 | 33页码:127749 |
| 关键词 | TNIK inhibitor 1H-pyrrolo[2,3-b]pyridine IL-2 secretion inhibitory |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2020.127749 |
| 文献子类 | Article |
| 英文摘要 | In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target. |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000615361300003 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309398]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhao, Dongmei; Miao, Zehong; Chen, Danqi |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Medial, Dept Med Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Medial, Div Antitumor Pharmacol, State Key Lab Drug Res, 501 Haike Rd, Shanghai 201203, Peoples R China; 3.Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Rd, Shenyang 110016, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Bowen,Wu, Qian,Huan, Xiajuan,et al. Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2021,33:127749. |
| APA | Yang, Bowen.,Wu, Qian.,Huan, Xiajuan.,Wang, Yingqing.,Sun, Yin.,...&Chen, Danqi.(2021).Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,33,127749. |
| MLA | Yang, Bowen,et al."Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 33(2021):127749. |
入库方式： OAI收割
来源：上海药物研究所
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