YM-254890 and FR900359 are potent and selective inhibitors of the Gq/11-signaling pathway. As such, they have been attractive targets for both synthesis and biological studies. Yet in spite of this effort, a versatile synthetic approach to the molecules that allows for the rapid construction of a variety of non-natural and labelled analogs and an increase in the amount of those analogs available remains elusive. We report here a convergent building block approach to the molecules that can solve this challenge.

Original languageEnglish
Article numbere202300365
JournalEuropean Journal of Organic Chemistry
Issue number20
StatePublished - May 22 2023


  • cyclic peptide synthesis
  • inhibitors
  • synthetic methods
  • total synthesi
  • YM-analogs


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