A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs

Lulu Zhao; Xinyu Yuan; Jubo Wang; Yifan Feng; Fei Ji; Zhiyu Li; Jinlei Bian

doi:10.1016/j.bmc.2019.01.027

A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs

Bioorg Med Chem. 2019 Mar 1;27(5):677-685. doi: 10.1016/j.bmc.2019.01.027. Epub 2019 Jan 26.

Authors

Lulu Zhao¹, Xinyu Yuan¹, Jubo Wang¹, Yifan Feng¹, Fei Ji¹, Zhiyu Li², Jinlei Bian³

Affiliations

¹ Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China.
² Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China. Electronic address: zhiyuli@cpu.edu.cn.
³ Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China. Electronic address: bianjl@cpu.edu.cn.

PMID: 30733087
DOI: 10.1016/j.bmc.2019.01.027

Abstract

Protein kinases have been important targets for antitumor targets due to their key roles in regulating multiple cell signaling pathways. Numerous compounds containing flavonoid scaffold as an indispensable anchor have been found to be potent inhibitors of protein kinases. Some of these flavonoids have been in clinical research as protein kinases inhibitors. Thus, the present review mainly focuses on the structural requirement for anticancer potential of flavone derivatives targeting several key serine/threonine protein kinases. This information may provide an opportunity to scientists of medicinal chemistry to design multi-functional flavone derivatives for the treatment of cancer.

Keywords: Binding mode; Cancer; Flavonoids; Protein kinase; Structure-activity relationship.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Animals
Antineoplastic Agents / chemistry
Antineoplastic Agents / metabolism
Antineoplastic Agents / therapeutic use*
Flavones / chemistry
Flavones / metabolism
Flavones / therapeutic use*
Humans
Neoplasms / drug therapy*
Protein Binding
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / metabolism
Protein Kinase Inhibitors / therapeutic use*
Protein Serine-Threonine Kinases / antagonists & inhibitors*
Protein Serine-Threonine Kinases / chemistry
Protein Serine-Threonine Kinases / metabolism

Substances

Antineoplastic Agents
Flavones
Protein Kinase Inhibitors
Protein Serine-Threonine Kinases