Synthesis and PPAR-gamma ligand-binding activity of the new series of 2'-hydroxychalcone and thiazolidinedione derivatives |
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Authors: | Jung Sang Hoon Park Soo Young Kim-Pak Youngmi Lee Hong Kyu Park Kyong Soo Shin Kuk Hyun Ohuchi Kazuo Shin Hyun-Kyung Keum Sam Rok Lim Soon Sung |
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Affiliation: | Natural Products Research Center, Korea Institute of Science and Technology, Seoul. |
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Abstract: | Fifteen chalcones and three thiazolidinedione (TZD) chalcones were prepared to evaluate their peroxisome proliferator-activated receptor-gamma (PPAR-gamma) ligand-binding activities. Among the three TZDs, one compound possessed PPAR-gamma transactivation potential, while the others showed antagonistic activity against PPAR-gamma transactivation. Among the chalcones, compound 5 was the most potent, and structure-activity relationship studies indicated that a methoxyl group in position C-4 and hydroxyl group in position C-4' or 5' in chalcone plays a key role in determining the potency of PPAR-gamma activation. |
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