Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity
文献类型：期刊论文
| 作者 | Yang, Chengbin1; Zhang, Xi2; Wang, Yi2; Yang, Yongtai1; Liu, Xiaofeng1; Deng, Mingli1; Jia, Yu1; Ling, Yun1; Meng, Ling-hua2 ; Zhou, Yaming1
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| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2017-08 |
| 卷号 | 8期号:8页码:875-880 |
| 关键词 | PI3K PI3K/mTOR oncology 1H-pyrrolo[2,3-b] pyridine cancer therapy |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/acsmedchemlett.7b00222 |
| 文献子类 | Article |
| 英文摘要 | The phosphoinositide 3-kinase (PI3K) inhibitors potently inhibit the signaling pathway of PI3K/AKT/mTOR, which provides a promising new approach for the molecularly targeted cancer therapy. In this work, a novel series of 7-azaindole scaffold derivatives was discovered by the fragment-based growing strategy. The structure-activity relationship profiles identified that the 7-azaindole scaffold derivatives exhibit potent activity against PI3K at molecular and cellular levels as well as cell proliferation in a panel of human tumor cells. |
| WOS关键词 | PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS ; (PI3K)/MAMMALIAN TARGET ; PI3K/AKT/MTOR PATHWAY ; ANTITUMOR-ACTIVITY ; KINASE INHIBITOR ; CANCER-THERAPY ; HIGHLY POTENT ; RAPAMYCIN ; IDENTIFICATION ; DESIGN |
| 资助项目 | NSFC[21471035] ; NSFC[81503109] ; Shanghai Leading Academic Discipline Project[B108] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000407656800016 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272541]  |
| 专题 | 药理学第一研究室 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 |
| 通讯作者 | Meng, Ling-hua; Zhou, Yaming |
| 作者单位 | 1.Fudan Univ, Shanghai Key Lab Mol Catalysis & Innovat Mat, Dept Chem, Shanghai 200433, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Chengbin,Zhang, Xi,Wang, Yi,et al. Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity[J]. ACS MEDICINAL CHEMISTRY LETTERS,2017,8(8):875-880. |
| APA | Yang, Chengbin.,Zhang, Xi.,Wang, Yi.,Yang, Yongtai.,Liu, Xiaofeng.,...&Zhou, Yaming.(2017).Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.ACS MEDICINAL CHEMISTRY LETTERS,8(8),875-880. |
| MLA | Yang, Chengbin,et al."Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity".ACS MEDICINAL CHEMISTRY LETTERS 8.8(2017):875-880. |
入库方式： OAI收割
来源：上海药物研究所
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