Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo [2,1-f] [1,2,4] triazine derivatives

被引：13

作者：

Xiang, Hao-Yue ^{[1
,2
]}

Chen, Yan-Hong ^{[2
]}

Wang, Yi ^{[2
]}

Zhang, Xi ^{[2
]}

Ding, Jian ^{[2
]}

Meng, Ling-Hua ^{[2
]}

Yang, Chun-Hao ^{[2
]}

机构：

[1] Cent South Univ, Coll Chem & Chem Engn, Changsha 410083, Hunan, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2020年 / 30卷 / 12期

基金：

中国国家自然科学基金;

关键词：

Antiproliferative; Cancer; Therapy; PI3K inhibitors; Pyrrolo [2,1-f][1,2,4] triazine; Kinase; SMALL-MOLECULE INHIBITORS; I PI3 KINASE; 3-KINASE; IDENTIFICATION; POTENT; DISCOVERY; PATHWAY;

D O I：

10.1016/j.bmcl.2020.127194

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 6-aminocarbonyl pyrrolo [2,1-f] [1,2,4]triazine derivatives were designed by scaffold hopping strategy. The IC50 values of compound 14a against PI3Ks were measured, showing selective activity against p110 alpha and p110 delta with IC(50)s of 122 nM and 119 nM respectively. All the synthesized compounds were evaluated for their antiproliferative activity against human cancer cells by SRB assay. Compounds 14a, 14p and 14q exhibited potent antiproliferative activity against five types of human cancer cells and the PK property of 14q was also investigated here.

引用

页数：4

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