Title of article :
Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase
Author/Authors :
Dale L. Boger، نويسنده , , Thomas H. Marsilje، نويسنده , , René A. Castro، نويسنده , , Michael P. Hedrick، نويسنده , , Qing-jin، Meng نويسنده , , Stephen J. Baker، نويسنده , , Jae Hoon Shim، نويسنده , , Stephen J. Benkovic، نويسنده ,
Abstract :
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.
