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

ABSTRACT: 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.

SUBMITTER: Paruch K 

PROVIDER: S-EPMC4007794 | biostudies-other | 2010 Aug

REPOSITORIES: biostudies-other

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

Paruch Kamil K   Dwyer Michael P MP   Alvarez Carmen C   Brown Courtney C   Chan Tin-Yau TY   Doll Ronald J RJ   Keertikar Kerry K   Knutson Chad C   McKittrick Brian B   Rivera Jocelyn J   Rossman Randall R   Tucker Greg G   Fischmann Thierry T   Hruza Alan A   Madison Vincent V   Nomeir Amin A AA   Wang Yaolin Y   Kirschmeier Paul P   Lees Emma E   Parry David D   Sgambellone Nicole N   Seghezzi Wolfgang W   Schultz Lesley L   Shanahan Frances F   Wiswell Derek D   Xu Xiaoying X   Zhou Quiao Q   James Ray A RA   Paradkar Vidyadhar M VM   Park Haengsoon H   Rokosz Laura R LR   Stauffer Tara M TM   Guzi Timothy J TJ  

ACS medicinal chemistry letters 20100517 5

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. ...[more]

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