Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 2: SAR of the acetylenic P1' group

Autor:	R. Cowling, Amy Sung, C.J March, Jeremy I. Levin, Roy A. Black, G. Jin, Frances C. Nelson, S. Skala, Dauphine Barone, James M. Chen, Kendall M. Mohler, Loran M. Killar, Mila T. Du, J.S. Skotnicki
Rok vydání:	2002
Předmět:	Stereochemistry Clinical Biochemistry Pharmaceutical Science ADAM17 Protein Hydroxamic Acids Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship In vivo Drug Discovery Moiety ortho-Aminobenzoates Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Sulfonamides Hydroxamic acid biology Acetylene Organic Chemistry Metalloendopeptidases In vitro Sulfonamide ADAM Proteins Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 12(8)
ISSN:	0960-894X
Popis:	The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors bearing novel acetylenic P1′ groups was explored. In particular, compound 4t bearing a butynyloxy P1′ moiety has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1 and oral activity in an in vivo model of TNF-α production.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b841da89ea8fcc430f56a96972ec73c https://pubmed.ncbi.nlm.nih.gov/11934588 Zobrazit plný text záznamu Full Text from ScienceDirect