Design, synthesis, and biological evaluation of simplified α-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase

Thomas H. Marsilje, Michael P. Hedrick, Joel Desharnais, Ali Tavassoli, Yan Zhang, Ian A. Wilson, Stephen J. Benkovic, Dale L. Boger

Research output: Contribution to journalArticlepeer-review

30 Scopus citations

Abstract

A series of simplified α-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues lacking the benzoylglutamate subunit were prepared and examined as potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase).

Original languageEnglish (US)
Pages (from-to)4487-4501
Number of pages15
JournalBioorganic and Medicinal Chemistry
Volume11
Issue number20
DOIs
StatePublished - Oct 1 2003

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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