Synthesis of desthio prenylcysteine analogs: sulfur is important for biological activity.

نویسندگان

  • Brian S Henriksen
  • Jessica L Anderson
  • Christine A Hrycyna
  • Richard A Gibbs
چکیده

N-Acetyl-S-farnesyl cysteine (AFC) is the minimal synthetic substrate for the enzyme Icmt, which methylates prenylated proteins. The desthio-AFC isostere 2 has been synthesized in racemic form. This analog was not an Icmt substrate, but instead a weak inhibitor with an IC50 of approximately 325 microM.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry letters

دوره 15 22  شماره 

صفحات  -

تاریخ انتشار 2005