CAS: 1357470-29-1; 8-Cyclopentyl-2-((4-(4-Methylpiperazin-1-yl)Phenyl)Amino)-7-Oxo-7,8-Dihydropyrido[2,3-D]Pyrimidine-6-Carbonitrile

📜4-氨基-2-甲巯基嘧啶-5-甲醛置于sodium Hydride,溶剂黄146,间氯过氧苯甲酸,苄胺体系中,用 二氯甲烷,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 11.08H,反应生成8-环戊基-7,8-二氢-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-7-氧代-吡啶并[2,3-D]嘧啶-6-甲腈
参考文献:Discovery Of 8-Cyclopentyl-2-[4-(4-Methyl-Piperazin-1-yl)-Phenylamino]-7-Oxo-7,8-Dihydro-Pyrido[2,3-D]Pyrimidine-6-Carbonitrile (7X) As A Potent Inhibitor Of Cyclin-Dependent Kinase 4 (Cdk4) And Ampk-Related Kinase 5 (Ark5)
标题:Discovery Of 8-Cyclopentyl-2-[4-(4-Methyl-Piperazin-1-yl)-Phenylamino]-7-Oxo-7,8-Dihydro-Pyrido[2,3-D]Pyrimidine-6-Carbonitrile (7X) As A Potent Inhibitor Of Cyclin-Dependent Kinase 4 (Cdk4) And Ampk-Related Kinase 5 (Ark5)
摘要:The Success Of Imatinib,A Bcr-Abl Inhibitor For The Treatment Of Chronic Myelogenous Leukemia,Has Created A Great Impetus For The Development Of Additional Kinase Inhibitors As Therapeutic Agents. However,The Complexity Of Cancer Has Led To Recent Interest In Polypharmacological Approaches For Developing Multikinase Inhibitors With Low Toxicity Profiles. With This Goal In Mind,We Analyzed More Than 150 Novel Cyano Pyridopyrimidine Compounds And Identified Structure-Activity Relationship Trends That Can Be Exploited In The Design Of Potent Kinase Inhibitors. One Compound,8-Cyclopentyl-2[-4-(4-Methyl-Piperazin-L-yl)-Phenylamino]-7-Oxo-7,8-Dihydro-Pyrido[2,3-D]Pyrimidine-6-Carbonitrile (7X),Was Found To Be The Most Active,Inducing Apoptosis Of Tumor Cells At A Concentration Of Approximately 30-100 Nm. In Vitro Kinase Profiling Revealed That 7X Is A Multikinase Inhibitor With Potent Inhibitory Activity Against The Cdk4/cyclin D1 And Arks Kinases. Here,We Report The Synthesis,Structure-Activity Relationship,Kinase Inhibitory Profile,In Vitro Cytotoxicity,And In Vivo Tumor Regression Studies By This Lead Compound.
Doi:10.1021/jm401073P

专利信息

专利号:US-9359298-B2
优先权日:2011-12-23
标题:Cajanine structure analogous compound, preparation method and use
发明人：LI ZHUORONG; JI XINGYUE; Xue situ; ZHENG GUANGHUI; LI YUHUAN; TAO PEIZHEN; JIANG JIANDONG
权利人:INST MED BIOTECHNOLOGY CAMS
摘要:Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.