Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl) benzamides as novel RET kinase inhibitors
文献类型：期刊论文
| 作者 | Han, Mei1; Li, Shan3; Ai, Jing2 ; Sheng, Rong3; Hu, Yongzhou3; Hu, Youhong4; Geng, Meiyu2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2016-12-01 |
| 卷号 | 26期号:23页码:5679-5684 |
| 关键词 | RET kinase inhibitor 1,2,4-Oxadiazole Anti-cancer therapy |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2016.10.061 |
| 文献子类 | Article |
| 英文摘要 | A series of novel 4-chloro-benzamides derivatives containing substituted five-membered heteroaryl ring were designed, synthesized and evaluated as RET kinase inhibitors for cancer therapy. Most of compounds exhibited moderate to high potency in ELISA-based kinase assay. In particular, compound I-8 containing 1,2,4-oxadiazole strongly inhibited RET kinase activity both in molecular and cellular level. In turn, I-8 inhibited cell proliferation driven by RET wildtype and gatekeeper mutation. The results implied that 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl) benzamides are promising lead compounds as novel RET kinase inhibitor for further investigation. (C) 2016 Elsevier Ltd. All rights reserved. |
| WOS关键词 | POTENT INHIBITOR ; LUNG-CANCER ; FUSIONS ; PONATINIB ; ALK |
| 资助项目 | Chinese National Science Foundation[81225022] ; Chinese National Science Foundation[81473243] ; Institutes for Drug Discovery and Development, Chinese Academy of Sciences[CASIMM0120162005] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000389519100013 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275786]  |
| 专题 | 药物化学研究室 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 药理学第一研究室 |
| 通讯作者 | Hu, Youhong; Geng, Meiyu |
| 作者单位 | 1.Ocean Univ China, Sch Med & Pharm, Dept Pharmacol & Glycobiol, Qingdao 266003, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 3.Zhejiang Univ, Coll Pharmaceut Sci, Zhejiang Prov Key Lab Anticanc Drug Res, ZJU ENS Joint Lab Med Chem, Hangzhou 310058, Zhejiang, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 ZuChongZhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Han, Mei,Li, Shan,Ai, Jing,et al. Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl) benzamides as novel RET kinase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016,26(23):5679-5684. |
| APA | Han, Mei.,Li, Shan.,Ai, Jing.,Sheng, Rong.,Hu, Yongzhou.,...&Geng, Meiyu.(2016).Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl) benzamides as novel RET kinase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,26(23),5679-5684. |
| MLA | Han, Mei,et al."Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl) benzamides as novel RET kinase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 26.23(2016):5679-5684. |
入库方式： OAI收割
来源：上海药物研究所
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