Identification of a potent and noncytotoxic inhibitor of melanin production |
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| Authors: | Soonho Hwang Sang Yoon Choi Jin Hee Lee Shinae Kim Jinkyung In Sang Keun Ha Eunjung Lee Tae-Yoon Kim Sun Yeou Kim Sun Choi Sanghee Kim |
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| Institution: | 1. College of Pharmacy, Seoul National University, San 56-1, Shilim, Kwanak, Seoul 151-742, Republic of Korea;2. Graduate School of East-West Medical Science, Kyunghee University, 1 Hoegi, Dongdaemun, Seoul 130-701, Republic of Korea;3. College of Pharmacy, Division of Life and Pharmaceutical Sciences, and National Core Research Center for Cell Signaling and Drug Discovery, Ewha Womans University, 11-1 Daehyun-Dong, Seodaemun, Seoul 120-750, Republic of Korea;4. Laboratory of Dermatology-Immunology, College of Medicine, The Catholic University of Korea, 505 Banpo, Seocho, Seoul 137-040, Republic of Korea |
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| Abstract: | On the basis of a hit from random screening, biaryl amide derivatives were prepared in a combinatorial manner via parallel solution-phase synthesis, and their effects on melanocytes were investigated to discover new effective skin depigmenting agents. Among the 120 derivatives prepared, five members exhibited a >30% reduction of melanin production at 30 μM with a cell viability of >90%. In particular, compound A3/B5 exhibited effective inhibitory activity on melanin synthesis. Although the inhibition percentage of A3/B5 was slightly lower than that of the positive reference compound, phenylthiourea (PTU), A3/B5 demonstrated a much better cell viability than PTU. In vivo evaluation of A3/B5 also showed a significant decrease of melanin pigments. In addition, the in silico classification model was built based on the experimental data of library members. Our results suggest that these biaryl amide derivatives may act as potent skin depigmenting agents. |
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