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Identification of a potent and noncytotoxic inhibitor of melanin production

Title
Identification of a potent and noncytotoxic inhibitor of melanin production
Authors
Hwang S.Choi S.Y.Lee J.H.Kim S.In J.Ha S.K.Lee E.Kim T.-Y.Kim S.Y.Choi S.
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2010
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 18, no. 15, pp. 5602 - 5609
Indexed
SCI; SCIE; SCOPUS WOS scopus
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 A 3/B 5 exhibited effective inhibitory activity on melanin synthesis. Although the inhibition percentage of A 3/B 5 was slightly lower than that of the positive reference compound, phenylthiourea (PTU), A 3/B 5 demonstrated a much better cell viability than PTU. In vivo evaluation of A 3/B 5 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. © 2010 Elsevier Ltd.
DOI
10.1016/j.bmc.2010.06.034
Appears in Collections:
약학대학 > 약학과 > Journal papers
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