N-Phenyl-N-purin-6-yl ureas: The design and synthesis of p38α MAP kinase inhibitors

Autor:	Zehong Wan, Jerry L. Adams, Shouki Kassis, Baoguang Zhao, John C. Lee, Jeffrey C. Boehm, Michael J. Bower
Rok vydání:	2003
Předmět:	Models Molecular Magnetic Resonance Spectroscopy Tertiary amine Molecular model Stereochemistry Clinical Biochemistry Molecular Conformation Pharmaceutical Science Crystallography X-Ray p38 Mitogen-Activated Protein Kinases Biochemistry Chemical synthesis Structure-Activity Relationship Drug Discovery Urea Structure–activity relationship Enzyme Inhibitors Protein kinase A Molecular Biology Bicyclic molecule biology Chemistry Kinase Purine Inhibitors Organic Chemistry General Medicine Pattern synthesis Enzyme inhibitor Drug Design Mitogen-activated protein kinase biology.protein Purine derivative Molecular Medicine Indicators and Reagents Mitogen-Activated Protein Kinases
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:1191-1194
ISSN:	0960-894X
Popis:	The design, synthesis and SAR of a series of 2,6,9-trisubstituted purine inhibitors of p38alpha kinase is reported. Synthetic routes were devised to allow for array synthesis in which all three points of diversity could be facilely explored. The binding of this novel series to p38alpha kinase, which was predicted to have several key interactions in common with SB-203580, was confirmed by X-ray crystallography of 19 (p38 IC(50)=82 nM).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54c8d5c487fe58e3cab4072d1aa1b14a https://doi.org/10.1016/s0960-894x(03)00048-9 Zobrazit plný text záznamu Full Text from ScienceDirect