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1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases
Raj N Misra1, David B Rawlins, Hai-yun Xiao
1Bristol-Myers Squibb Pharmaceutical Research Institute, PO 4000, Princeton, NJ 08543-4000, USA.
Bioorganic & Medicinal Chemistry Letters
|March 20, 2003
Abstract:
1H-Pyrazolo[3,4-b]pyridine 3 (SQ-67563) has been shown to be a potent, selective inhibitor of CDK1/CDK2 in vitro. In cells 3 acts as a cytotoxic agent with the ability to block cell cycle progression and/or induce apoptosis. The solid state structure of 3 bound to CDK2 shows 3 resides coincident with the ATP purine binding site and forms important H-bonding interactions with Leu83 on the protein backbone.