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10-formyl-5,8,10-trideazafolic acid (10-formyl-TDAF): a potent inhibitor of glycinamide ribonucleotide transformylase

Academic Article
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Overview

related to degree

  • Haynes, Nancy-Ellen, Ph.D. in Organic Chemistry, Scripps Research 1991 - 1996

authors

  • Boger, Dale
  • Haynes, Nancy-Ellen
  • Kitos, P. A.
  • Warren, M. S.
  • Ramcharan, J.
  • Marolewski, A. E.
  • Benkovic, S. J.

publication date

  • September 1997

journal

  • Bioorganic & Medicinal Chemistry  Journal

abstract

  • The synthesis of 10-formyl-5,8,10-trideazafolic acid (3) as a potential inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) is reported. The target compound was prepared by a convergent synthesis utilizing the alkylation of hydrazone 5 with benzylic bromide 6 to construct the core heterocycle 7. The aldehyde 3 and related agents were evaluated as inhibitors of purN GAR Tfase and avian AICAR Tfase. Compound 3 exhibited potent inhibition of GAR Tfase with a Ki of 0.26 +/- 0.05 microM. In contrast, 3 exhibited more moderate inhibition of aminoimidazole carboxamide ribonucleotide transformylase (AICAR Tfase), with Ki of 7.6 +/- 1.5 microM.

subject areas

  • Cell Division
  • Drug Design
  • Enzyme Inhibitors
  • Humans
  • Hydroxymethyl and Formyl Transferases
  • Kinetics
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Phosphoribosylglycinamide Formyltransferase
  • Spectrometry, Mass, Fast Atom Bombardment
  • Tumor Cells, Cultured
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Identity

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/s0968-0896(97)00120-x

PubMed ID

  • 9354237
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Additional Document Info

start page

  • 1817

end page

  • 1830

volume

  • 5

issue

  • 9

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