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Prostaglandin photoaffinity probes: Synthesis and binding affinity of C-18 substituted PGF(2α) prostanoids bearing a perfluorinated aryl azide

  • M. Golinski
  • , M. Heine
  • , D. J. Orlicky
  • , T. A. Fitz
  • , D. S. Watt

Producción científica: Articlerevisión exhaustiva

1 Cita (Scopus)

Resumen

C-18 Phenoxy analogs of prostaglandin F(2α) (PGF(2α)) that possessed a perfluorinated aryl azide and an aryl iodide sustituent were synthesized and evaluated as potential photoaffinity probes for PGF(2α). Prior studies indicated that only hydrophobic modifications in the ω-side chain of PGF(2α) were compatible with high binding affinity, and this finding excluded the use of a hydroxyl-substituted C-18 phenoxy group as an activated aryl ring capable of radioiodination. Consequently, an alternate means of introducing the iodine substituent using an ipso-substitution of a trimethylsilyl arene was developed. Although this strategy was successful from a synthetic perspective, the potential PGF(2α) photoaffinity probe, (15S)-18-[3'-((4''-azide-2'',3'',5'',6''- tetrafluorophenyl)methoxy)methyl-5'-iodophenoxy]-19,20-bisnorprostaglandin F(2α), exhibited only marginal competitive binding with [3H]-PGF(2α) to ovine luteal cells and to plasma membranes of bovine corpora lutea. The hydrophobic but bulky C-18 substituent was presumably incompatible with effective receptor binding.

Idioma originalEnglish
Páginas (desde-hasta)87-97
Número de páginas11
PublicaciónEicosanoids
Volumen5
N.º2
EstadoPublished - 1992

Financiación

FinanciadoresNúmero del financiador
Eunice Kennedy Shriver National Institute of Child Health and Human DevelopmentR01HD025961

    ASJC Scopus subject areas

    • Biochemistry
    • Pharmacology

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