Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 1, Pages 362-372Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b01431
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Funding
- Project of National Science Foundation of China [81473436, 81402822]
- Project of International Cooperation Plan from Ministry of Science and Technology of China [2015DFG32260]
- State Key Program of National Natural Science of China [U1508221]
- Strategic Priority Research Program of the Chinese Academy of Sciences, Personalized Medicines-Molecular Signature-based Drug Discovery and Development [XDA12040314]
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A family of 2H-chromen-2-one derivatives were identified as G protein-coupled receptor-35 (GPR35) agonists using dynamic mass redistribution assays in HT-29 cells. The compounds with 1H-tetrazol-5-y1 in 3-substituted position displayed higher potency than the corresponding carboxyl analogs, and the hydroxyl group in the 7-position also played an important role in GPR35 agonistic activity. 6-Bromo-7-hydroxy-8-nitro-3-(1H-tetrazol-5-71)-2H-chromen-2-one (50) was found to be the most potent GPR35 agonist with an EC50 of 5.8 nM. Calculating the physicochemical properties of compounds with moderate to high potency suggested that compounds 30, 50, and 51 showed good druggability. This study provides a novel series of GPR35 agonists, and compound 50 may be a powerful tool to study GPR35.
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