Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide

Authors
Shahripour, AB Plummer, MS Lunney, EA Sawyer, TK Stankovic, CJ Connolly, MK Rubin, JR Walker, NPC Brady, KD Allen, HJ Talanian, RV Wong, WW Humblet, C
Citation
Ab. Shahripour et al., Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide, BIOORG MED, 11(20), 2001, pp. 2779-2782
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
20
Year of publication
2001
Pages
2779 - 2782
Database
ISI
SICI code
0960-894X(20011022)11:20<2779:SDOCIC>2.0.ZU;2-4
Abstract
A series of compounds was designed and prepared as inhibitors of interleuki n-1 beta converting enzyme (ICE), also known as caspase-1. These inhibitors , which employ a diphenyl ether sulfonamide, were designed to improve poten cy by forming favorable interactions between the diphenyl ether rings and t he prime side hydrophobic region. An X-ray crystal structure of a represent ative member of the diphenyl ether sulfonamide series bound to the active s ite of caspase-1 was obtained. (C) 2001 Elsevier Science Ltd. All rights re served.