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

doi:10.1016/j.bmcl.2011.11.003

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	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
	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
	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.
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关键词	3-KINASES ; CANCER ; POTENT ; PTEN
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000298636700064
内容类型	期刊论文
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.