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

被引：11

作者：

Boger, DL

Marsilje, TH

Castro, RA

Hedrick, MP

Jin, Q

Baker, SJ

Shim, JH

Benkovic, SJ

机构：

[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA

[2] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA

[3] Penn State Univ, Dept Chem, University Pk, PA 16802 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(00)00271-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The examination results of a novel series of potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. These agents incorporate an electrophilic fluoronitrophenyl group that can potentially react with an active site nucleophile or the substrate GAR/AICAR amine via nucleophilic aromatic substitution. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：1471 / 1475

页数：5

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