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Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors |
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| Authors: | Dwyer Michael P Paruch Kamil Alvarez Carmen Doll Ronald J Keertikar Kerry Duca Jose Fischmann Thierry O Hruza Alan Madison Vincent Lees Emma Parry David Seghezzi Wolfgang Sgambellone Nicole Shanahan Frances Wiswell Derek Guzi Timothy J |
| Institution: | Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. michael.dwyer@spcorp.com |
| 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 pyrazolo1,5-a]pyrimidine core (represented by 9) emerged as the superior core for further elaboration in the identification of novel CDK2 inhibitors. |
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