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SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists
- Authors
- Yoon, Dong-Oh; Zhao, Xiaodi; Son, Dohyun; Han, Jung Tae; Yun, Jaesook; Shin, Dongyun; Park, Hyun-Ju
- Issue Date
- Dec-2017
- Publisher
- AMER CHEMICAL SOC
- Keywords
- GPR40 agonists; indole-5-propanoic acid; NFAT reporter assay; glucose-stimulated insulin secretion (GSIS)
- Citation
- ACS MEDICINAL CHEMISTRY LETTERS, v.8, no.12, pp.1336 - 1340
- Journal Title
- ACS MEDICINAL CHEMISTRY LETTERS
- Volume
- 8
- Number
- 12
- Start Page
- 1336
- End Page
- 1340
- ISSN
- 1948-5875
- Abstract
- G-protein coupled receptor 40 (GPR40) has been considered to be an attractive drug target for the treatment of type 2 diabetes because of its role in free fatty acids-mediated enhancement of glucose-stimulated insulin secretion (GSIS) from pancreatic beta-cells. A series of indole-5-propanoic acid compounds were synthesized, and their GPR40 agonistic activities were evaluated by nuclear factor of activated T-cells reporter assay and GSIS assay in the MIN-6 insulinoma cells. Three compounds, 8h (EC50 = 58.6 nM), 8i (EC50 = 37.8 nM), and 8o (EC50 = 9.4 nM), were identified as potent GPR40 agonists with good GSIS effects.
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Related Researcher
- Shin, Dong Yun
- Pharmacy (Dept.of Pharmacy)