1H-pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases

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 wit...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-03, Vol.13 (6), p.1133-1136
Hauptverfasser:	MISRA, Raj N, RAWLINS, David B, WEBSTER, Kevin R, XIAO, Hai-Yun, WEIFANG SHAN, BURSUKER, Isia, KELLAR, Kristin A, MULHERON, Janet G, SACK, John S, TOKARSKI, John S, KIMBALL, S. David
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Biological and medical sciences Biological Assay CDC2 Protein Kinase - antagonists & inhibitors CDC2-CDC28 Kinases Cell Cycle - drug effects Cyclin-Dependent Kinase 2 Cyclin-Dependent Kinases - antagonists & inhibitors Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Female General aspects Humans Hydrogen Bonding Medical sciences Models, Molecular Molecular Conformation Ovarian Neoplasms - drug therapy Pharmacology. Drug treatments Protein-Serine-Threonine Kinases - antagonists & inhibitors Pyrazoles - chemical synthesis Pyrazoles - pharmacology Pyridines - chemical synthesis Pyridines - pharmacology Structure-Activity Relationship Tumor Cells, Cultured
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00034-9