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Inventi Impact: Med Chem

Articles

  • Inventi:pmc/29334/19
    Evaluation and Optimization of the Anti-Melanogenic Activity of 1-(2-Cyclohexylmethoxy-6- Hydroxy-phenyl)-3-(4-Hydroxymethyl-phenyl)-Propenone Derivatives
    Research 2019 : July - September
    Byung-Hak Kim, Soo-Nam Hong, Sang-Kyu Ye, Jung-Youl Park

    The chemical modification and optimization of biologically active compounds are\nessential steps in the identification of promising lead compounds for drug development. We\npreviously reported the anti-melanogenic activity of 1-(2-cyclohexylmethoxy-6-hydroxy-phenyl)-\n3-(4-hydroxymethyl-phenyl)-propenone (chalcone 21). In this study, we synthesized 21 derivatives\nof chalcone 21 and evaluated their anti-melanogenic activity in alpha -MSH-induced B16F10 cells. (E)-\nN-(4-(3-(2-(Cyclohexylmethoxy)phenyl)-3-oxoprop-1-en-1-yl)phenyl)acetamide (chalcone 21-21)\nexhibited the strongest inhibition of cellular melanin production, with an IC50 value of 0.54Micro M. It\nwas more potent than chalcone 21 and the known anti-melanogenic agents kojic acid and arbutin,\nwhose IC50 values were 4.9, 38.5, and 148.4 Micro M, respectively. Chalcone 21-21 decreased the\nexpression and activity of tyrosinase. It also decreased the expression of TRP1, TRP2 and MITF,\nthe phosphorylation of CREB and ERK1/2, and the transcriptional activity of MITF and CRE. Our\nresults demonstrate that chalcone-21-21 is an effective lead compound with anti-melanogenic\nactivity.

    How to Cite this Article
    Attribution/ CC Compliant Citation: Kim, Byung-Hak, et al. \"Evaluation and Optimization of the Anti-Melanogenic\nActivity of 1-(2-Cyclohexylmethoxy-6-hydroxy-phenyl)-3-(4-hydroxymethyl-phenyl)-propenone Derivatives.\"\nMolecules 24.7 (2019): 1372.\nhttps://doi:10.3390/molecules24071372\nhttp://creativecommons.org/licenses/by/4.0/\n\nSome formatting elements, header, footer, logos, dates and pagination were modified while adapting this article.
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