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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Sonawane YA,Zhu Y,Garrison JC,Ezell EL,Zahid M,Cheng X,Natarajan Adoi
10.1021/acsmedchemlett.7b00358subject
Has Abstractpub_date
2017-10-02 00:00:00pages
1183-1187issue
11issn
1948-5875journal_volume
8pub_type
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