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

Tao Liu; Zhongmiao Xu; Qiaojun He; Yanhong Chen; Bo Yang; Yongzhou Hu

doi:10.1016/j.bmcl.2006.07.088

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

Bioorg Med Chem Lett. 2007 Jan 1;17(1):278-81. doi: 10.1016/j.bmcl.2006.07.088. Epub 2006 Nov 7.

Authors

Tao Liu¹, Zhongmiao Xu, Qiaojun He, Yanhong Chen, Bo Yang, Yongzhou Hu

Affiliation

¹ ZJU-ENS Joint Laboratory of Medicinal Chemistry, School of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, PR China.

PMID: 17085048
DOI: 10.1016/j.bmcl.2006.07.088

Abstract

A novel series of nitrogen-containing flavonoids 5a-l, 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.

MeSH terms

CDC2 Protein Kinase / antagonists & inhibitors*
Cell Proliferation / drug effects
Cells, Cultured
Cyclin B / antagonists & inhibitors*
Drug Design
Flavonoids / chemical synthesis
Flavonoids / chemistry*
Flavonoids / pharmacology*
Humans
Nitrogen / chemistry
Protein Kinase Inhibitors / chemical synthesis
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / pharmacology*

Substances

Cyclin B
Flavonoids
Protein Kinase Inhibitors
CDC2 Protein Kinase
Nitrogen