Novel phosphate mimetics for the design of non-peptidyl inhibitors of protein tyrosine phosphatases

Authors
Kotoris, CC Chen, MJ Taylor, SD
Citation
Cc. Kotoris et al., Novel phosphate mimetics for the design of non-peptidyl inhibitors of protein tyrosine phosphatases, BIOORG MED, 8(22), 1998, pp. 3275-3280
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
22
Year of publication
1998
Pages
3275 - 3280
Database
ISI
SICI code
0960-894X(19981117)8:22<3275:NPMFTD>2.0.ZU;2-Y
Abstract
Benzylic alpha,alpha-difluorosulfonates, alpha,alpha-dinuorotetrazoles, and alpha,alpha-difluorocarboxylates of type 5 and 6 were synthesized and exam ined as potential phosphate biosteres for PTP1B inhibition. The alpha,alpha -difluorosulfonates and alpha,alpha-difluorotetrazoles were found to be mor e effective inhibitors than the analogous compounds bearing the fluoromalon yl group, a phosphate biostere currently being used for PTP inhibition. (C) 1998 Elsevier Science Ltd. All rights reserved.