Discovery and bioactivity of 4-(2-arylpyrido[3 ',2 ':3,4]pyrrolo[1,2-f][1,2,4]-triazin-4-yl) morpholine derivatives as novel PI3K inhibitors
文献类型：期刊论文
| 作者 | Wang, Jia ; Wang, Xiang; Chen, Yanhong; Chen, Simeng; Chen, Guang; Tong, Linjiang; Meng, Linghua; Xie, Yuyuan; Ding, Jian; Yang, Chunhao
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012 |
| 卷号 | 22期号:1页码:339-342 |
| 关键词 | PI3K Cancer PI-103 analogs |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2011.11.003 |
| 文献子类 | Article |
| 英文摘要 | PI3K is a promising therapeutic target for cancer. With PI-103 as the lead compound, we designed and synthesized 4-(2-arylpyrido[3',2':3,4] pyrrolo[1,2-f][1,2,4]triazin-4-yl)morpholine derivatives. 9, 10a, 10d, 10e had the IC50 against PI3K alpha comparable with PI-103. All of the compounds showed selectivity over 15 tested protein kinases and anti-proliferative activity at micromolar concentration against several cancer cell lines. (C) 2011 Elsevier Ltd. All rights reserved. |
| WOS关键词 | 3-KINASES ; CANCER ; POTENT ; PTEN |
| 资助项目 | National Natural Science Foundation of China[20772138] ; National Natural Science Foundation of China[90713034] ; National Natural Science Foundation of China[81021062] ; Shanghai Municipality Science and Technology Development Fund[09JC1416600] ; Chinese Academy of Sciences[KSCX2-EW-Q-3] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000298636700064 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278279]  |
| 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 药物化学研究室 国家新药筛选中心 |
| 通讯作者 | Meng, Linghua |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, SIBS, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Jia,Wang, Xiang,Chen, Yanhong,et al. Discovery and bioactivity of 4-(2-arylpyrido[3 ',2 ':3,4]pyrrolo[1,2-f][1,2,4]-triazin-4-yl) morpholine derivatives as novel PI3K inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(1):339-342. |
| APA | Wang, Jia.,Wang, Xiang.,Chen, Yanhong.,Chen, Simeng.,Chen, Guang.,...&Yang, Chunhao.(2012).Discovery and bioactivity of 4-(2-arylpyrido[3 ',2 ':3,4]pyrrolo[1,2-f][1,2,4]-triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(1),339-342. |
| MLA | Wang, Jia,et al."Discovery and bioactivity of 4-(2-arylpyrido[3 ',2 ':3,4]pyrrolo[1,2-f][1,2,4]-triazin-4-yl) morpholine derivatives as novel PI3K inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.1(2012):339-342. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。