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

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.

SUBMITTER: Sonawane YA 

PROVIDER: S-EPMC5774307 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature

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

Sonawane Yogesh A YA   Zhu Yingmin Y   Garrison Jered C JC   Ezell Edward L EL   Zahid Muhammad M   Cheng Xiaodong X   Natarajan Amarnath A  

ACS medicinal chemistry letters 20171002 11

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 <b>12a</b> exists as a mixture of inseparable <i>E</i> (major) and <i>Z</i> (minor) rotamers. The rotation about the <i>N</i>-formyl group  ...[more]

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