title: Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.
abstract: A series of four bicyclic cores were prepared and evaluated as cyclin-dependent kinase-2 (CDK2) inhibitors. From the in-vitro and cell-based analysis, the pyrazolo[1,5-a]pyrimidine core (represented by 9) emerged as the superior core for further elaboration in the identification of novel CDK2 inhibitors.
authors: Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. michael.dwyer@spcorp.com
authors: Michael P
authors: MP
authors: Dwyer
authors: Kamil
authors: K
authors: Paruch
authors: Carmen
authors: C
authors: Alvarez
authors: Ronald J
authors: RJ
authors: Doll
authors: Kerry
authors: K
authors: Keertikar
authors: Jose
authors: J
authors: Duca
authors: Thierry O
authors: TO
authors: Fischmann
authors: Alan
authors: A
authors: Hruza
authors: Vincent
authors: V
authors: Madison
authors: Emma
authors: E
authors: Lees
authors: David
authors: D
authors: Parry
authors: Wolfgang
authors: W
authors: Seghezzi
authors: Nicole
authors: N
authors: Sgambellone
authors: Frances
authors: F
authors: Shanahan
authors: Derek
authors: D
authors: Wiswell
authors: Timothy J
authors: TJ
authors: Guzi
mesh_terms: D001665:Binding Sites; D018360:Crystallography, X-Ray; D051357:Cyclin-Dependent Kinase 2 / Q000737:chemistry / Q000187:drug effects*; D050756:Cyclin-Dependent Kinase Inhibitor Proteins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D050756:Cyclin-Dependent Kinase Inhibitor Proteins; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D011743:Pyrimidines; C527752:pyrazolo(1,5-a)pyrimidine; D051357:Cyclin-Dependent Kinase 2