2. Academic Validation
  3. Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase

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

  • Bioorg Med Chem Lett. 2000 Jul 3;10(13):1471-5. doi: 10.1016/s0960-894x(00)00271-7.
D L Boger 1,  T H Marsilje,  R A Castro,  M P Hedrick,  Q Jin,  S J Baker,  J H Shim,  S J Benkovic
Affiliations

Affiliation

  • 1 Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, CA 92037, USA. boger@scripps.edu
PMID: 10888335 DOI: 10.1016/s0960-894x(00)00271-7
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.

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