Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B
文献类型：期刊论文
| 作者 | Chen, Hai-Jun; Liu, Yong; Wang, Li-Na; Shen, Qiang; Li, Jia ; Nan, Fa-Jun
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2010-05-01 |
| 卷号 | 20期号:9页码:2876-2879 |
| 关键词 | Structural optimization Cdc25B inhibitor Pyrazole derivatives |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2010.03.040 |
| 文献子类 | Article |
| 英文摘要 | Structural optimization and preliminary structure-activity relationship studies of a series of N-substituted maleimide fused-pyrazole analogues with Cdc25B inhibitory activity, starting from a high-throughput screening hit, are illustrated. A simplified 3,5-diacyl pyrazole analogue was obtained as the most potent compound (118, IC50 = 0.12 mu M) with a 270-fold increase in potency. (C) 2010 Elsevier Ltd. All rights reserved. |
| WOS关键词 | PHOSPHATASE INHIBITORS ; BIOLOGICAL EVALUATION ; CANCER-CELLS ; TYROSINE ; ANALOGS ; HOMOLOG ; LIBRARY ; FAMILY |
| 资助项目 | National Natural Science Foundation of China[30725049] ; National Natural Science Foundation of China[30801406] ; National Natural Science Foundation of China[30721005] ; National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program', China[2009ZX09301-001] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000276816600039 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278905]  |
| 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 药物安全性评价中心 |
| 通讯作者 | Li, Jia |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drugs Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Hai-Jun,Liu, Yong,Wang, Li-Na,et al. Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(9):2876-2879. |
| APA | Chen, Hai-Jun,Liu, Yong,Wang, Li-Na,Shen, Qiang,Li, Jia,&Nan, Fa-Jun.(2010).Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(9),2876-2879. |
| MLA | Chen, Hai-Jun,et al."Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.9(2010):2876-2879. |
入库方式： OAI收割
来源：上海药物研究所
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