227617-18-7Relevant academic research and scientific papers
USE OF PYRAZOLO [3,4-b] PYRIDINE AS CYCLIN DEPENDANT KINASE INHIBITORS
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Page/Page column 13, (2010/11/26)
Compounds of the formula and pharmaceutically acceptable salts thereof for use as inhibitors of cyclin dependent kinases, wherein: X is O, S(O)m; Y is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl; R1 is hydrogen or lower alkyl; R2 is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -O-alkyl, -O-aryl, -NR4R5; R3 is hydrogen or lower alkyl; R4 is hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -O-alkyl, -O-aryl; R5 is hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, cycloalkyl, alkylcycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, -O-alkyl, -O-aryl; and m is 0, 1 or 2. The compounds of formula I are protein kinase inhibitors and are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.
1H-pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: Highly potent 2,6-difluorophenacyl analogues
Misra, Raj N.,Xiao, Hai-Yun,Rawlins, David B.,Shan, Weifang,Kellar, Kristen A.,Mulheron, Janet G.,Sack, John S.,Tokarski, John S.,Kimball, S. David,Webster, Kevin R.
, p. 2405 - 2408 (2007/10/03)
Structure-activity studies of 1H-pyrazolo[3,4-b]pyridine 1 have resulted in the discovery of potent CDK1/CDK2 selective inhibitor 21h, BMS-265246 (CDK1/cycB IC50=6 nM, CDK2/cycE IC50=9 nM). The 2,6-difluorophenyl substitution was cri
