264141-05-1Relevant academic research and scientific papers
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4- d]pyrimidin-4-one inhibitors of cyclin-dependent kinases
Markwalder, Jay A.,Arnone, Marc R.,Benfield, Pamela A.,Boisclair, Michael,Burton, Catherine R.,Chang, Chong-Hwan,Cox, Sarah S.,Czerniak, Philip M.,Dean, Charity L.,Doleniak, Deborah,Grafstrom, Robert,Harrison, Barbara A.,Kaltenbach III, Robert F.,Nugiel, David A.,Rossi, Karen A.,Sherk, Susan R.,Sisk, Lisa M.,Stouten, Pieter,Trainor, George L.,Worland, Peter,Seitz, Steven P.
, p. 5894 - 5911 (2007/10/03)
Using a high-throughput screening strategy, a series of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]-pyrimidin-4-ones was identified that inhibit the cyclin-dependent kinase (CDK) 4/cyclin D1 complex-mediated phosphorylation of a protein substrate with IC50
6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
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, (2008/06/13)
The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
