2. Academic Validation
  3. Functionalized N,N-Diphenylamines as Potent and Selective EPAC2 Inhibitors

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

  • ACS Med Chem Lett. 2016 Mar 28;7(5):460-4. doi: 10.1021/acsmedchemlett.5b00477.
Christopher T Wild 1,  Yingmin Zhu 2,  Ye Na 1,  Fang Mei 2,  Marcus A Ynalvez 1,  Haiying Chen 1,  Xiaodong Cheng 2,  Jia Zhou 1
Affiliations

Affiliations

  • 1 Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch , Galveston, Texas 77555, United States.
  • 2 Department of Integrative Biology and Pharmacology and Texas Therapeutics Institute, University of Texas Health Science Center , Houston, Texas 77030, United States.
PMID: 27190593 DOI: 10.1021/acsmedchemlett.5b00477
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.

Keywords

Buchwald−Hartwig amination; Exchange proteins directly activated by cAMP (EPAC) inhibitors; diphenylamines; structure−activity relationship.

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