Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases

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...

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Published inACS medicinal chemistry letters Vol. 1; no. 5; pp. 204 - 208
Main Authors Paruch, Kamil, Dwyer, Michael P, Alvarez, Carmen, Brown, Courtney, Chan, Tin-Yau, Doll, Ronald J, Keertikar, Kerry, Knutson, Chad, McKittrick, Brian, Rivera, Jocelyn, Rossman, Randall, Tucker, Greg, Fischmann, Thierry, Hruza, Alan, Madison, Vincent, Nomeir, Amin A, Wang, Yaolin, Kirschmeier, Paul, Lees, Emma, Parry, David, Sgambellone, Nicole, Seghezzi, Wolfgang, Schultz, Lesley, Shanahan, Frances, Wiswell, Derek, Xu, Xiaoying, Zhou, Quiao, James, Ray A, Paradkar, Vidyadhar M, Park, Haengsoon, Rokosz, Laura R, Stauffer, Tara M, Guzi, Timothy J
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 12.08.2010
Subjects
Letter
Cyclin-dependent kinase
SCH 727965
oncology therapeutics
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Summary: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.
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Merck Research Laboratories, 320 Bent Street, Cambridge, Massachusetts 02141.
Novartis Institute for Biomedical Research, 4560 Horton Street, Emeryville, California 94608-2916.
Department of Chemistry, Masaryk University, Kamenice 5, 625 00 Brno, Czech Republic.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml100051d