@article{a8b3410b8828494e97238c03af1093db,
title = "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.",
keywords = "dynamic NMR, exchange protein directly activated by cAMP, rotamer, tetrahydroquinoline",
author = "Sonawane, {Yogesh A.} and Yingmin Zhu and Garrison, {Jered C.} and Ezell, {Edward L.} and Muhammad Zahid and Xiaodong Cheng and Amarnath Natarajan",
note = "Funding Information: *Tel: (402) 559-3793. Fax: (402) 559-8270. E-mail: anatarajan@unmc.edu. ORCID Yogesh A. Sonawane: 0000-0002-6799-7525 Jered C. Garrison: 0000-0002-8376-9821 Amarnath Natarajan: 0000-0001-5067-0203 Funding A.N. is supported by the Eppley Pilot Grant, Fred and Pamela Buffett Cancer Center Support Grant from NIH (P30CA036727). X.C. is supported by funding from NIH (R01GM066170 and R35GM122536). Notes The authors declare no competing financial interest. Publisher Copyright: {\textcopyright} 2017 American Chemical Society.",
year = "2017",
month = nov,
day = "9",
doi = "10.1021/acsmedchemlett.7b00358",
language = "English (US)",
volume = "8",
pages = "1183--1187",
journal = "ACS Medicinal Chemistry Letters",
issn = "1948-5875",
publisher = "American Chemical Society",
number = "11",
}