Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase

Authors
Boger, DL Marsilje, TH Castro, RA Hedrick, MP Jin, Q Baker, SJ Shim, JH Benkovic, SJ
Citation
Dl. Boger et al., Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase, BIOORG MED, 10(13), 2000, pp. 1471-1475
Citations number
29
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
13
Year of publication
2000
Pages
1471 - 1475
Database
ISI
SICI code
0960-894X(20000703)10:13<1471:DSABEO>2.0.ZU;2-M
Abstract
The examination results of a novel series of potential inhibitors of glycin amide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxam ide transformylase (AICAR Tfase) are reported. These agents incorporate an electrophilic fluoronitrophenyl group that can potentially react with an ac tive site nucleophile or the substrate GAR/AICAR amine via nucleophilic aro matic substitution. (C) 2000 Elsevier Science Ltd. All rights reserved.