Identification of Indoline-2-thione Analogs as Novel Potent Inhibitors of α-Melanocyte Stimulating Hormone Induced Melanogenesis

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概要

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• Based on the hits, 3,4-dihydroquinazoline-2-thione (1) and benzimidazole-2-thione (2), a series of indole-2-thione (3) and indole-2-thiol inhibitors (4) of melanogenesis were designed, synthesized and evaluated in melanoma B16 cells under the stimulant of α-melanocyte stimulating hormone (α-MSH). The indole-2-thione compounds (3a—g) exhibited an effective inhibitory activity on melanin synthesis. The Structure–Activity Relationship (SAR) studies of 2 have revealed that in potent inhibitor 3a (>100% inhibition at 30 μM, IC50=1.40 μM) the role of nitrogen (3-N) at 3-position is insignificance. In addition, the hydrophobic substituents of 3 were better than the hydrophilic one. However, conversion of thione (–C=S, 3) to thiol (–C–SH, 4) led to decrease in the potency.

著者

• Jung Sang-hun

  College Of Pharmacy Chungnam National University

• Kim Youngsoo

  College Of Pharmacy & Research Center For Bioresource And Health Chungbuk National University

• Thanigaimalai Pillaiyar

  College of Pharmacy and Institute of Drug Research and Development, Chungnam National University

• Lee Ki-Cheul

  College of Pharmacy and Institute of Drug Research and Development, Chungnam National University

• Sharma Vinay

  College of Pharmacy and Institute of Drug Research and Development, Chungnam National University

• Roh Eunmiri

  College Of Pharmacy Chungbuk National University

• Sharma Niti

  College of Pharmacy and Institute of Drug Research and Development, Chungnam National University

• Jung Sang-Hun

  College of Pharmacy and Institute of Drug Research and Development, Chungnam National University

関連論文

• Novel Benzo[d]imidazole-2(3H)-thiones as Potent Inhibitors of the α-Melanocyte Stimulating Hormone Induced Melanogenesis in Melanoma B16 Cells
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• Anti-inflammatory Benzene Diamine Compound Inhibited Toll-Like Receptor 4-Mediated Inducible Nitric Oxide Synthase Expression and Nuclear Factor-KappaB Activation(Pharmacology)
• Identification of Indoline-2-thione Analogs as Novel Potent Inhibitors of α-Melanocyte Stimulating Hormone Induced Melanogenesis
• α-Viniferin Suppresses the Signal Transducer and Activation of Transcription-1 (STAT-1)-Inducible Inflammatory Genes in Interferon-γ-Stimulated Macrophages

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