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Design, Synthesis and Preliminary Biological Evaluation of Purine-2,6-diamine Derivatives as Cyclin-dependent Kinase (CDK) Inhibitors
Wang, Junhua1; Wang, Quande1; Zhang, Liangren2; Fang, Hao1
关键词purine derivatives CDK inhibitors antitumor agents regulation of cell cycle
刊名CHINESE JOURNAL OF CHEMISTRY
2013-09-01
DOI10.1002/cjoc.201300420
31期:9页:1181-1191
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary
研究领域[WOS]Chemistry
关键词[WOS]CELL-CYCLE ; ROSCOVITINE ; CANCER ; POTENT ; MICE ; PROGRESS ; PURINE
英文摘要

Novel purine-2,6-diamine derivatives were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. 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 11a (IC50=0.35 mu mol/L for CDK1/cyclin B and IC50=0.023 mu mol/L for CDK2/cyclin A) possessed better inhibitory effect compared with Roscovitine (IC50=2.54 (mol/L for CDK1/cyclin B and IC50=0.092 mu mol/L for CDK2/cyclin A).

语种英语
WOS记录号WOS:000327882900010
项目编号21172133 ; ZR2010HM028 ; NCET-12-0337 ; 2012JC003 ; K20100107
资助机构National Natural Foundation Research Grant ; Shandong Provincial Natural Science Foundation ; Program for New Century Excellent Talents in University ; Independent Innovation Foundation of Shandong University (IIFSDU) ; Open Research Fund of State Key Laboratory of Natural and Biomimetic Drugs in Peking University
引用统计
被引频次:7[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/63403
专题北京大学药学院
北京大学药学院_药物化学系
作者单位1.Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Jinan 250012, Shandong, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Wang, Junhua,Wang, Quande,Zhang, Liangren,et al. Design, Synthesis and Preliminary Biological Evaluation of Purine-2,6-diamine Derivatives as Cyclin-dependent Kinase (CDK) Inhibitors[J]. CHINESE JOURNAL OF CHEMISTRY,2013,31(9):1181-1191.
APA Wang, Junhua,Wang, Quande,Zhang, Liangren,&Fang, Hao.(2013).Design, Synthesis and Preliminary Biological Evaluation of Purine-2,6-diamine Derivatives as Cyclin-dependent Kinase (CDK) Inhibitors.CHINESE JOURNAL OF CHEMISTRY,31(9),1181-1191.
MLA Wang, Junhua,et al."Design, Synthesis and Preliminary Biological Evaluation of Purine-2,6-diamine Derivatives as Cyclin-dependent Kinase (CDK) Inhibitors".CHINESE JOURNAL OF CHEMISTRY 31.9(2013):1181-1191.
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