Document Report Card
Basic Information
ID: ALA4130621
Journal: ACS Med Chem Lett
Title: Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors.
Authors: Sonawane YA, Zhu Y, Garrison JC, Ezell EL, Zahid M, Cheng X, Natarajan A.
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.
CiteXplore: 29375750