Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors
文献类型：期刊论文
| 作者 | Song, Pinrao1; Peng, Peng1; Han, Mengmeng2; Cao, Xianchao2; Ma, Xiaodong1; Liu, Tao1; Zhou, Yubo2 ; Hu, Yongzhou1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2014-09-01 |
| 卷号 | 22期号:17页码:4882-4892 |
| 关键词 | Chk1 inhibitor Thienopyridinones Antitumor Cell synergy |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2014.06.044 |
| 文献子类 | Article |
| 英文摘要 | A series of thienopyridinone derivatives was designed and synthesized as inhibitors of checkpoint kinase 1 (Chk1). Most of them exhibited moderate to good Chk1 inhibitory activities. Among them, compounds 8q, 8t, and 8w with excellent Chk1 inhibitory activities (IC50 values of 4.05, 6.23, and 2.33 nM, respectively) displayed strong synergistic effects with melphalan, a DNA-damaging agent in the cell-based assay. Further kinase profiling indicated that compound 8t was highly selective against CDK2/cyclinA, Aurora A, and PKC. Crown Copyright (C) 2014 Published by Elsevier Ltd. All rights reserved. |
| WOS关键词 | POTENT ; CHECKPOINT ; KINASE ; DISCOVERY ; ACTIVATION ; AZD7762 |
| 资助项目 | National Natural Science Foundation of China[81172929] ; Program for Zhejiang Leading Team of ST Innovation[2011R50014] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000341293300038 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276927]  |
| 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 药物化学研究室 |
| 通讯作者 | Liu, Tao |
| 作者单位 | 1.Zhejiang Univ, ZJU ENS Joint Lab Med Chem, Zhejiang Prov Key Lab Anticanc Drug Res, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Song, Pinrao,Peng, Peng,Han, Mengmeng,et al. Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2014,22(17):4882-4892. |
| APA | Song, Pinrao.,Peng, Peng.,Han, Mengmeng.,Cao, Xianchao.,Ma, Xiaodong.,...&Hu, Yongzhou.(2014).Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,22(17),4882-4892. |
| MLA | Song, Pinrao,et al."Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 22.17(2014):4882-4892. |
入库方式： OAI收割
来源：上海药物研究所
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