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ACS Med Chem Lett. 2017 Oct 02;8(11):1183-1187. doi: 10.1021/acsmedchemlett.7b00358. eCollection 2017 Nov 09.

Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors.

ACS medicinal chemistry letters

Yogesh A Sonawane, Yingmin Zhu, Jered C Garrison, Edward L Ezell, Muhammad Zahid, Xiaodong Cheng, Amarnath Natarajan

Affiliations

  1. Eppley Institute for Research in Cancer and Allied Diseases, Fred and Pamela Buffett Cancer Center, Departments of Pharmaceutical Sciences, Environmental, Agricultural and Occupational Health, and Genetics Cell Biology and Anatomy, University of Nebraska Medical Center, Omaha, Nebraska 68022, 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: 29375750 PMCID: PMC5774307 DOI: 10.1021/acsmedchemlett.7b00358

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

Conflict of interest statement

The authors declare no competing financial interest.

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