Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594516 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
5,6,7,8-Tetrahydro-4H-cyclohepta[d]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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Authors
Jiho Song, Hyun-e Lee, Young Jin Kim, Su Yeon Kim, Dong-Seok Kim, Kyung Hoon Min,