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

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TY  - JOUR
  - Paruch, K.,Dwyer, M. P.,Alvarez, C.,Brown, C.,Chan, T. Y.,Doll, R. J.,Keertikar, K.,Knutson, C.,McKittrick, B.,Rivera, J.,Rossman, R.,Tucker, G.,Fischmann, T.,Hruza, A.,Madison, V.,Nomeir, A. A.,Wang, Y.,Kirschmeier, P.,Lees, E.,Parry, D.,Sgambellone, N.,Seghezzi, W.,Schultz, L.,Shanahan, F.,Wiswell, D.,Xu, X.,Zhou, Q.,James, R. A.,Paradkar, V. M.,Park, H.,Rokosz, L. R.,Stauffer, T. M.,Guzi, T. J.
  - 2010
  - August
  - Acs Med Chem Lettacs Med Chem Lett
  - Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases
  - Validated
  - ()
  - 1
  - 5
  - 204
  - 208
  - 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.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.
  - 1948-58751948-5875
DA  - 2010/08
ER  - 
@article{V280546814,
   = {Paruch,  K. and Dwyer,  M. P. and Alvarez,  C. and Brown,  C. and Chan,  T. Y. and Doll,  R. J. and Keertikar,  K. and Knutson,  C. and McKittrick,  B. and Rivera,  J. and Rossman,  R. and Tucker,  G. and Fischmann,  T. and Hruza,  A. and Madison,  V. and Nomeir,  A. A. and Wang,  Y. and Kirschmeier,  P. and Lees,  E. and Parry,  D. and Sgambellone,  N. and Seghezzi,  W. and Schultz,  L. and Shanahan,  F. and Wiswell,  D. and Xu,  X. and Zhou,  Q. and James,  R. A. and Paradkar,  V. M. and Park,  H. and Rokosz,  L. R. and Stauffer,  T. M. and Guzi,  T. J. },
   = {2010},
   = {August},
   = {Acs Med Chem Lettacs Med Chem Lett},
   = {Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases},
   = {Validated},
   = {()},
   = {1},
   = {5},
  pages = {204--208},
   = {{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.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.}},
  issn = {1948-58751948-5875},
  source = {IRIS}
}
AUTHORSParuch, K.,Dwyer, M. P.,Alvarez, C.,Brown, C.,Chan, T. Y.,Doll, R. J.,Keertikar, K.,Knutson, C.,McKittrick, B.,Rivera, J.,Rossman, R.,Tucker, G.,Fischmann, T.,Hruza, A.,Madison, V.,Nomeir, A. A.,Wang, Y.,Kirschmeier, P.,Lees, E.,Parry, D.,Sgambellone, N.,Seghezzi, W.,Schultz, L.,Shanahan, F.,Wiswell, D.,Xu, X.,Zhou, Q.,James, R. A.,Paradkar, V. M.,Park, H.,Rokosz, L. R.,Stauffer, T. M.,Guzi, T. J.
YEAR2010
MONTHAugust
JOURNAL_CODEAcs Med Chem Lettacs Med Chem Lett
TITLEDiscovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases
STATUSValidated
TIMES_CITED()
SEARCH_KEYWORD
VOLUME1
ISSUE5
START_PAGE204
END_PAGE208
ABSTRACTInhibition 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.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.
PUBLISHER_LOCATION
ISBN_ISSN1948-58751948-5875
EDITION
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