3 years ago

Structure–Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors

Structure–Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors
Jered C. Garrison, Yogesh A. Sonawane, Amarnath Natarajan, Yingmin Zhu, Edward L. Ezell, Xiaodong Cheng, Muhammad Zahid
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.

Publisher URL: http://dx.doi.org/10.1021/acsmedchemlett.7b00358

DOI: 10.1021/acsmedchemlett.7b00358

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