4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

Autor:	Heather Hobbs, Rick P. C. Cousins, Caroline Whitworth, Ruth R. Osborn, Cesar Ramirez-Molina, Giorgia Vicentini, Chris Ioannou, Chun-wa Chung, Jeremy John Payne, Michelle L. Heathcote, Michael David Barker, Sebastien Andre Campos, Paul Faulder, Mary A. Morse, William L. Rumsey, John Liddle, Daniel Terence Tape, John Martin Pritchard, Rick Williamson, Duncan S. Holmes, Paul Bamborough
Rok vydání:	2012
Předmět:	Indoles Neutrophils Clinical Biochemistry Rat model Biological Availability Pharmaceutical Science Pharmacology Biochemistry Structure-Activity Relationship In vivo Drug Discovery Animals Humans Transferase Lung Protein Kinase Inhibitors Molecular Biology Whole blood Chemistry Kinase Organic Chemistry I-kappa B Kinase Rats Bioavailability Disease Models Animal Molecular Medicine Selectivity Half-Life
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 22:5222-5226
ISSN:	0960-894X
Popis:	The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery of 16, a potent and selective IKK2 inhibitor showing good efficacy in a rat model of neutrophil activation.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66c01094b7cd1f9f02ade498d99ac86e https://doi.org/10.1016/j.bmcl.2012.06.065 Zobrazit plný text záznamu Full Text from ScienceDirect