Functionalized N,N-Diphenylamines as Potent and Selective EPAC2 Inhibitors

Christopher T. Wild, Yingmin Zhu, Ye Na, Fang Mei, Marcus A. Ynalvez, Haiying Chen, Xiaodong Cheng, Jia Zhou

Research output: Contribution to journalArticle

9 Scopus citations

Abstract

N,N-Diphenylamines were discovered as potent and selective EPAC2 inhibitors. A study was conducted to determine the structure-activity relationships in a series of inhibitors of which several compounds displayed submicromolar potencies. Selectivity over the related EPAC1 protein was also demonstrated. Computational modeling reveals an allosteric site that is distinct from the cAMP binding domain shared by both EPAC isoforms, providing a theory with regards to subtype selectivity.

Original languageEnglish (US)
Pages (from-to)460-464
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume7
Issue number5
DOIs
StatePublished - May 12 2016

Keywords

  • Buchwald-Hartwig amination
  • Exchange proteins directly activated by cAMP (EPAC) inhibitors
  • diphenylamines
  • structure-activity relationship

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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