Discovery of small molecules that inhibit melanogenesis via regulation of tyrosinase expression |
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Authors: | Jiho Song Hyun-e Lee Young Jin Kim Su Yeon Kim Dong-Seok Kim Kyung Hoon Min |
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Institution: | 1. College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea;2. Department of Biochemistry, Chung-Ang University College of Medicine, Seoul 156-756, Republic of Korea |
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Abstract: | 5,6,7,8-Tetrahydro-4H-cycloheptad]isoxazole derivatives were synthesized and evaluated as a novel class of inhibitors for α-melanocyte-stimulating hormone (α-MSH) induced melanogenesis in a mouse melanoma B16F10 cell line. Compound 8e (IC50 = 0.67 μM), 8h (IC50 = 1.01 μM) and 9b (IC50 = 0.99 μM) exhibited a potent inhibitory activity approximately 85- to 126-fold greater than kojic acid, a well-known potent inhibitor. A biochemical study indicates that the activity of this series should be displayed via down-regulation of the expression of tyrosinase. |
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