Nitrogen-containing flavonoids as CDK1/Cyclin B inhibitors: Design, synthesis, and biological evaluation

被引：27

作者：

Liu, Tao

Xu, Zhongmiao

He, Qiaojun

Chen, Yanhong

Yang, Bo

Hu, Yongzhou ^{[1
]}

机构：

[1] Zhejiang Univ, Sch Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310031, Peoples R China

[2] Zhejiang Univ, Sch Pharmaceut Sci, Dept Pharmacol, Hangzhou 310031, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 01期

关键词：

cyclin-dependent kinases (CDKs) inhibitor; antiproliferative activity; flavonoids; apoptosis;

D O I：

10.1016/j.bmcl.2006.07.088

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of nitrogen-containing flavonoids 5a-1, 6a,b, and 7a,b were designed and synthesized as cyclin-dependent kinases (CDKs) inhibitors. The representative compounds 5a, 5b, 5e, and 5g showed potent CDK1/Cyclin B inhibitory activities. All compounds displayed a significant growth inhibitory action in vitro against Bel-7402, PC-3, ECA-109, A-549, HL-60, and MCF-7 cancer cell lines. Flow cytometry analysis showed that 5b induced apoptosis in PC-3 cells. (c) 2006 Published by Elsevier Ltd.

引用

页码：278 / 281

页数：4

共 18 条

[1]

Bu XY, 1997, SYNTHESIS-STUTTGART, P1246

[2]

Gulati K.C., 1943, ORG SYNTH, V2, P522

[3] Cyclin-dependent kinases [J].