Art

J-GLOBAL ID：201402264680805988   Reference number：14A0451006

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)

サイクリン依存的キナーゼ4(CDK4)およびAMPK関連キナーゼ5(ARK5)の強力阻害剤としての8-シクロペンチル-2-[4-(4-メチル-ピペラジン-1-イル)-フェニルアミノ]-7-オキソ-7,8-ジヒドロ-ピリド[2,3-d]ピリミジン-6-カルボニトリル(7x)の発見

Author (13)： REDDY M.V.Ramana (Icahn School of Medicine at Mount Sinai, New York, USA) ,  AKULA Balireddy (Onconova Therapeutics Inc., Pennsylvania, USA) ,  COSENZA Stephen C. (Icahn School of Medicine at Mount Sinai, New York, USA) ,  ATHULURIDIVAKAR Saikrishna (Icahn School of Medicine at Mount Sinai, New York, USA) ,  MALLIREDDIGARI Muralidhar R. (Onconova Therapeutics Inc., Pennsylvania, USA) ,  PALLELA Venkat R. (Onconova Therapeutics Inc., Pennsylvania, USA) ,  BILLA Vinay K. (Icahn School of Medicine at Mount Sinai, New York, USA) ,  SUBBAIAH D.R.C.Venkata (Icahn School of Medicine at Mount Sinai, New York, USA) ,  BHARATHI E.Vijaya (Icahn School of Medicine at Mount Sinai, New York, USA) ,  VASQUEZ-DEL CARPIO Rodrigo (Icahn School of Medicine at Mount Sinai, New York, USA) ,  PADGAONKAR Amol (Icahn School of Medicine at Mount Sinai, New York, USA) ,  BAKER Stacey J. (Icahn School of Medicine at Mount Sinai, New York, USA) ,  REDDY E.Premkumar (Icahn School of Medicine at Mount Sinai, New York, USA)
Material： Journal of Medicinal Chemistry  (J Med Chem)
Volume： 57  Issue： 3  Page： 578-599  Publication year： Feb. 13, 2014 
JST Material Number： D0102A  ISSN： 0022-2623  CODEN： JMCMAR  Document type： Article
Article type： 原著論文  Country of issue： United States (USA)  Language： ENGLISH (EN)

Thesaurus term： screening(inspection) ,  chemical synthesis ,  K562 cell ,  tumor cell ,  cultured cell ,  *cyclin-dependent kinase ,  *enzyme inhibitor ,  in vitro experiment ,  mouse(animal) ,  breast tumor ,  experimental disease ,  intraperitoneal administration ,  in vivo experiment ,  nitrogen heterocyclic compound ,  structure-activity relationship ,  drug design ,  molecular model ,  *antitumor drug ,  computer simulation
Semi thesaurus term： *ARK5 ,  *Cdk4 kinase ,  *cdk inhibitor ,  DU-145 cell ,  Pyrimidines ,  compound library ,  Molecular Docking Simulation ,  drug screening ,  drug synthesis

JST classification (2)： Basic research of antitumor(=antineoplastic)drugs  (GW16010A) ,  Pyrimidines  (CF07103W)

Substance index (1)： 8-Cyclopentyl-2-[4-(4-methyl-piperazine-1-yl)-phenylamino]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile

Terms in the title (10)： サイクリン ,  キナーゼ ,  Cdk4 ,  AMPK ,  ARK5 ,  阻害剤 ,  ピペラジン ,  ピリミジン ,  カルボニトリル ,  発見