Cyclin dependent kinase (CDK) inhibitors as anticancer drugs

被引：213

作者：

Sanchez-Martinez, Concepcion ^{[1
]}

Gelbert, Lawrence M. ^{[2
]}

Jose Lallena, Maria ^{[1
]}

de Dios, Alfonso ^{[3
]}

机构：

[1] Eli Lilly & Co, Discovery Chem Res & Technol, Alcobendas 28108, Madrid, Spain

[2] Indiana Univ, Herman B Wells Ctr Pediat Res, Sect Pediat Hematol Oncol, Indianapolis, IN 46202 USA

[3] Eli Lilly & Co, Discovery Chem Res & Technol, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 17期

关键词：

CDK inhibitors; Cell cycle; CELL-CYCLE; ANTITUMOR-ACTIVITY; CANCER-THERAPY; IN-VITRO; POTENT; DISCOVERY; COMBINATION; IDENTIFICATION; OPTIMIZATION; PEPTIDES;

D O I：

10.1016/j.bmcl.2015.05.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Sustained proliferative capacity is a hallmark of cancer. In mammalian cells proliferation is controlled by the cell cycle, where cyclin-dependent kinases (CDKs) regulate critical checkpoints. CDK4 and CDK6 are considered highly validated anticancer drug targets due to their essential role regulating cell cycle progression at the G1 restriction point. This review provides an overview of recent advances on cyclin dependent kinase inhibitors in general with special emphasis on CDK4 and CDK6 inhibitors and compounds under clinical evaluation. Chemical structures, structure activity relationships, and relevant preclinical properties will be described. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：3420 / 3435

页数：16

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