1.
ACS Med Chem Lett
; 1(5): 204-8, 2010 Aug 12.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24900195
RESUMO
Inhibition of cyclin-dependent kinases (CDKs) has emerged as an attractive strategy for the development of novel oncology therapeutics. Herein is described the utilization of an in vivo screening approach with integrated efficacy and tolerability parameters to identify candidate CDK inhibitors with a suitable balance of activity and tolerability. This approach has resulted in the identification of SCH 727965, a potent and selective CDK inhibitor that is currently undergoing clinical evaluation.
2.
Bioorg Med Chem Lett
; 17(22): 6220-3, 2007 Nov 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17904841
RESUMO
Properly substituted pyrazolo[1,5-a]pyrimidines are potent and selective CDK2 inhibitors. Compound 15j is orally available and showed efficacy in a mouse A2780 xenograft model.