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

被引：17

作者：

Wang, Jia ^{[1
]}

Wang, Xiang ^{[1
]}

Chen, Yanhong ^{[1
]}

Chen, Simeng ^{[1
]}

Chen, Guang ^{[1
]}

Tong, Linjiang ^{[1
]}

Meng, Linghua ^{[1
]}

Xie, Yuyuan ^{[1
]}

Ding, Jian ^{[1
]}

Yang, Chunhao ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, SIBS, Shanghai 201203, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 01期

基金：

中国国家自然科学基金;

关键词：

PI3K; Cancer; PI-103; analogs; 3-KINASES; CANCER; POTENT; PTEN;

D O I：

10.1016/j.bmcl.2011.11.003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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.

引用

页码：339 / 342

页数：4