Design, Synthesis and Preliminary Biological Evaluation of Purine-2,6-diamine Derivatives as Cyclin-dependent Kinase （CDK） Inhibitors  

作　　者：Junhua Wang Quande Wang Liangren Zhang Hao Fang 

机构地区：[1]Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, China [2]State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China

出　　处：《Chinese Journal of Chemistry》2013年第9期1181-1191,共11页中国化学（英文版）

基　　金：the National Natural Foundation Research Grant，the Shandong Provincial Natural Science Foundation，the Program for New Century Excellent Talents in University，Independent Innovation Foundation of Shandong University，the Open Research Fund of State Key Laboratory of Natural and Biomimetic Drugs in Peking University

摘　　要：Novel purine-2,6-diamine derivatives were designed and synthesized as cyclin-dependent kinase （CDK） inhibi- tors. According to the preliminary biological evaluation, most of the compounds show good inhibitory activities in CDK1 enzyme assay and potent antiproliferative activities in some tumor cell lines. Especially, compound lla （IC50=0.35 μmol/L for CDK1/cyclin B and IC50： effect compared with Roscovitine （IC50= 2.54 CDK2/cyclin A）. 0.023 μmol/L for CDK2/cyclin A） possessed better inhibitory μmol/L for CDK1/cyclin B and IC50=0.092 μ mol/L forNovel purine-2,6-diamine derivatives were designed and synthesized as cyclin-dependent kinase （CDK） inhibi- tors. According to the preliminary biological evaluation, most of the compounds show good inhibitory activities in CDK1 enzyme assay and potent antiproliferative activities in some tumor cell lines. Especially, compound lla （IC50=0.35 μmol/L for CDK1/cyclin B and IC50： effect compared with Roscovitine （IC50= 2.54 CDK2/cyclin A）. 0.023 μmol/L for CDK2/cyclin A） possessed better inhibitory μmol/L for CDK1/cyclin B and IC50=0.092 μ mol/L for

关 键 词：purine derivatives CDK inhibitors antitumor agents regulation of cell cycle 

分 类 号：Q253[生物学—细胞生物学] X826[环境科学与工程—环境工程]