1H-Pyrazolo[3,4-b]pyridine Inhibitors of Cyclin-Dependent Kinases

Bioorganic & Medicinal Chemistry Letters
2003.0

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.

Knowledge Graph

Similar Paper

1H-Pyrazolo[3,4-b]pyridine Inhibitors of Cyclin-Dependent Kinases
Bioorganic & Medicinal Chemistry Letters 2003.0
Pyrazolo[3,4-c]pyridazines as Novel and Selective Inhibitors of Cyclin-Dependent Kinases
Journal of Medicinal Chemistry 2005.0
Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 2003.0
Crystal Structure of Human Cyclin-Dependent Kinase 2 in Complex with the Adenine-Derived Inhibitor H717
Journal of Medicinal Chemistry 2001.0
Synthesis and Biological Evaluation of 1-Aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one Inhibitors of Cyclin-Dependent Kinases
Journal of Medicinal Chemistry 2004.0
A Novel Series of Highly Potent 2,6,9-Trisubstituted Purine Cyclin-Dependent Kinase Inhibitors
Journal of Medicinal Chemistry 2013.0
Pyrrolo[2,3-a]carbazoles as Potential Cyclin Dependent Kinase 1 (CDK1) Inhibitors. Synthesis, Biological Evaluation, and Binding Mode through Docking Simulations
Journal of Medicinal Chemistry 2008.0
Cyclin-Dependent Kinase Inhibition by New C-2 Alkynylated Purine Derivatives and Molecular Structure of a CDK2−Inhibitor Complex
Journal of Medicinal Chemistry 2000.0
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases
European Journal of Medicinal Chemistry 2016.0
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors
Bioorganic & Medicinal Chemistry 2011.0