Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2

Autor:	Alan Robertson, Justin Bower, Andrew Cansfield, Pawel Dokurno, James B. Murray, Jonathan D. Moore, Jenifer Powles, Geraint L. Francis, Richard Hebdon, Martin J. Parratt, Andrea M. Lockie, Douglas S. Williamson, Philip Stephen Jackson, Allan E. Surgenor, Christopher J. Torrance, Claire L. Nunns, Christine M. Richardson, Rob Howes
Rok vydání:	2004
Předmět:	Models Molecular Clinical Biochemistry Pharmaceutical Science Biochemistry Pyrazolopyrimidine chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship Cyclin-dependent kinase Cell Line Tumor Drug Discovery CDC2 Protein Kinase CDC2-CDC28 Kinases Humans Protein kinase A Molecular Biology Cell Proliferation Cyclin-dependent kinase 1 biology Kinase Organic Chemistry Cyclin-dependent kinase 2 Cyclin-Dependent Kinase 2 Pyrimidines chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Signal transduction
Zdroj:	Bioorganicmedicinal chemistry letters. 15(4)
ISSN:	0960-894X
Popis:	The protein structure guided design of a series of pyrazolo[1,5-a]pyrimidines with high potency for human cyclin-dependent kinase 2 (CDK2) is described. Some examples were shown to inhibit the growth of human colon tumour cells, were equipotent for CDK1 and were selective against GSK-3β and other kinases.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26ec504ae5ca00b08ec6dc13e0e3a860 https://pubmed.ncbi.nlm.nih.gov/15686876 Zobrazit plný text záznamu Full Text from ScienceDirect