Design, Synthesis and Preliminary Biological Evaluation of Purine-2,6-diamine Derivatives as Cyclin-dependent Kinase （CDK） Inhibitors
Design, Synthesis and Preliminary Biological Evaluation of Purine-2,6-diamine Derivatives as Cyclin-dependent Kinase （CDK） Inhibitors作者机构：Department of Medicinal Chemistry School of Pharmaceutical Sciences Shandong University Jinan Shandong 250012 China State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical Sciences Peking University Beijing 100191 China
出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)
年 卷 期：2013年第31卷第9期
页 面：1181-1191页
核心收录：
学科分类：0710[理学-生物学] 083002[工学-环境工程] 0830[工学-环境科学与工程（可授工学、理学、农学学位）] 07[理学] 08[工学] 071009[理学-细胞生物学] 09[农学] 0703[理学-化学] 0901[农学-作物学] 090102[农学-作物遗传育种] 0713[理学-生态学]
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
主 题：purine derivatives CDK inhibitors antitumor agents regulation of cell cycle
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 for
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