4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors

Autor:	Jeremy John Payne, Geoff W. Mellor, Smith Kathryn Jane, Richard A. Williamson, Sebastien Andre Campos, Geoffrey J. Cutler, Caroline Whitworth, Mary A. Morse, Michael David Barker, Heather Hobbs, Rick P. C. Cousins, Duncan S. Holmes, Daniel Terence Tape, Paul Bamborough, John Martin Pritchard, John Liddle, Chris Ioannou
Rok vydání:	2009
Předmět:	Models Molecular Cellular activity Indoles Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Pharmaceutical Science Tumor cells Biochemistry Chemical synthesis Inhibitory Concentration 50 Structure-Activity Relationship Adenosine Triphosphate Drug Discovery Humans Molecular Biology Tumor necrosis factor α chemistry.chemical_classification Sulfonamides Binding Sites Molecular Structure Kinase Organic Chemistry In vitro Sulfonamide I-kappa B Kinase Enzyme chemistry Models Chemical Drug Design Molecular Medicine Protein Binding
Zdroj:	Bioorganicmedicinal chemistry letters. 19(9)
ISSN:	1464-3405
Popis:	The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modification around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bac9d3089c47e68ac4f0cac67941fe59 https://pubmed.ncbi.nlm.nih.gov/19349179 Zobrazit plný text záznamu Full Text from ScienceDirect