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  • Title: 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.
    Author: Misra RN, Rawlins DB, Xiao HY, Shan W, Bursuker I, Kellar KA, Mulheron JG, Sack JS, Tokarski JS, Kimball SD, Webster KR.
    Journal: Bioorg Med Chem Lett; 2003 Mar 24; 13(6):1133-6. PubMed ID: 12643928.
    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.
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