11 Scopus citations

Abstract

EPAC proteins are therapeutic targets for the potential treatment of cardiac hypertrophy and cancer metastasis. Several laboratories use a tetrahydroquinoline analog, CE3F4, to dissect the role of EPAC1 in various disease states. Here, we report SAR studies with tetrahydroquinoline analogs that explore various functional groups. The most potent EPAC inhibitor 12a exists as a mixture of inseparable E (major) and Z (minor) rotamers. The rotation about the N-formyl group indeed impacts the activity against EPAC.

Original languageEnglish (US)
Pages (from-to)1183-1187
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume8
Issue number11
DOIs
StatePublished - Nov 9 2017

Keywords

  • dynamic NMR
  • exchange protein directly activated by cAMP
  • rotamer
  • tetrahydroquinoline

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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