title: Recent progress of cyclin-dependent kinase inhibitors as potential anticancer agents.
abstract: Deregulation of the cell cycle is a common feature in human cancer. The inhibition of cyclin-dependent kinases (CDKs), which play a crucial role in control of the cell cycle, has always been one of the most promising areas in cancer chemotherapy. This review first summarizes the biology of CDKs and then focuses on the recent advances in both broad-range and selective CDK inhibitors during the last 5 years. The design rationale, structural optimization and structure-activity relationships analysis of these small molecules have been discussed in detail and the key interactions with the amino-acid residues of the most important compounds are highlighted. Future perspectives for CDKs inhibitors will be defined in the development of highly selective CDK inhibitors, an accurate knowledge of gene control mechanism and further predictive biomarker research.
authors: Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing, 210009, China.|Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors: Tinghan
authors: T
authors: Li
authors: Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing, 210009, China.|Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors: Tianwei
authors: T
authors: Weng
authors: Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing, 210009, China.|Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors: Minzan
authors: M
authors: Zuo
authors: Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing, 210009, China.|Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors: Zhihui
authors: Z
authors: Wei
authors: Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing, 210009, China.|Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors: Ming
authors: M
authors: Chen
authors: Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing, 210009, China.|Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
authors: Zhiyu
authors: Z
authors: Li
keywords: cancer therapy; cell cycle; clinical trials; cyclin-dependent kinases; small-molecule inhibitors; structure–activity relationships