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SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-11-28 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00460 Dong-Oh Yoon , Xiaodi Zhao , Dohyun Son , Jung Tae Han , Jaesook Yun , Dongyun Shin 1 , Hyun-Ju Park
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-11-28 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00460 Dong-Oh Yoon , Xiaodi Zhao , Dohyun Son , Jung Tae Han , Jaesook Yun , Dongyun Shin 1 , Hyun-Ju Park
Affiliation
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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 β-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.
中文翻译：
吲哚-5-丙酸衍生物的SAR研究以开发新型GPR40激动剂
G蛋白偶联受体40（GPR40）被认为是治疗2型糖尿病的有吸引力的药物靶标，因为它在游离脂肪酸介导的胰岛β细胞葡萄糖刺激的胰岛素分泌（GSIS）的增强中发挥作用。合成了一系列吲哚-5-丙酸化合物，并通过MIN-6胰岛素瘤细胞中活化的T细胞报道分子分析和GSIS分析评估了它们的GPR40激动活性。鉴定出三种化合物，即8h（EC 50 = 58.6 nM），8i（EC 50 = 37.8 nM）和8o（EC 50 = 9.4 nM），是具有良好GSIS效应的有效GPR40激动剂。
更新日期：2017-11-28
中文翻译：
吲哚-5-丙酸衍生物的SAR研究以开发新型GPR40激动剂
G蛋白偶联受体40（GPR40）被认为是治疗2型糖尿病的有吸引力的药物靶标，因为它在游离脂肪酸介导的胰岛β细胞葡萄糖刺激的胰岛素分泌（GSIS）的增强中发挥作用。合成了一系列吲哚-5-丙酸化合物，并通过MIN-6胰岛素瘤细胞中活化的T细胞报道分子分析和GSIS分析评估了它们的GPR40激动活性。鉴定出三种化合物，即8h（EC 50 = 58.6 nM），8i（EC 50 = 37.8 nM）和8o（EC 50 = 9.4 nM），是具有良好GSIS效应的有效GPR40激动剂。
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