Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold
文献类型：期刊论文
| 作者 | Song, Pinrao1; Chen, Ming1; Ma, Xiaodong1; Xu, Lei2; Liu, Tao1; Zhou, Yubo2 ; Hu, Yongzhou1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-04-15 |
| 卷号 | 23期号:8页码:1858-1868 |
| 关键词 | Pyrrolopyridin-indazoles Antiproliferative agents Cell cycle profile Aurora A inhibitors Selectivity |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2015.02.004 |
| 文献子类 | Article |
| 英文摘要 | A novel series of 3-(pyrrolopyridin-2-yl)indazole derivatives were synthesized and biologically evaluated for their anti-proliferative effects on five human cancer cell lines. As a result, all of them exhibited vigorous potency against HL60 cell line with IC50 values ranging from singe digital nanomolar to micromolar level. Besides, a majority of them displayed modest to good antiproliferative activities against the other four cell lines, including KB, SMMC-7721, HCT116, and A549. Particularly, compound 2y, as the most distinguished one in this series, demonstrated IC50 values of 8.3 nM and 1.3 nM against HL60 and HCT116 cell lines, respectively. Afterwards, for exploring the molecular target, compounds 2d, 2g and 2y were further selected to evaluate the inhibitory activities against a panel of kinases. Finally, they were identified to be targeting Aurora A kinase with significant selectivity over other kinases, such as CHK1, CDK2, MEK1, GSK3 beta, BRAF, IKK beta and PKC. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | CELL-CYCLE KINASES ; CANCER ; THERAPY |
| 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:000351852400019 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276572]  |
| 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, Coll Pharmaceut Sci, Zhejiang Prov Key Lab Anticanc Drug Res, ZJU ENS Joint Lab Med Chem, 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,Chen, Ming,Ma, Xiaodong,et al. Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(8):1858-1868. |
| APA | Song, Pinrao.,Chen, Ming.,Ma, Xiaodong.,Xu, Lei.,Liu, Tao.,...&Hu, Yongzhou.(2015).Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold.BIOORGANIC & MEDICINAL CHEMISTRY,23(8),1858-1868. |
| MLA | Song, Pinrao,et al."Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold".BIOORGANIC & MEDICINAL CHEMISTRY 23.8(2015):1858-1868. |
入库方式： OAI收割
来源：上海药物研究所
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