Evaluation of 3,4-dihydroquinazoline-2(1H)-thiones as inhibitors of α-MSH-induced melanin production in melanoma B16 cells

P. Thanigaimalai, Ki Cheul Lee, Seong Cheol Bang, Jee Hyun Lee, Cheong Yong Yun, Eunmiri Roh, Bang Yeon Hwang, Youngsoo Kim, Sang Hun Jung

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37 Scopus citations

Abstract

Novel 3,4-dihydroquinazoline-2(1H)-thiones (QNTs) 1 were found to be potent inhibitors of α-MSH-induced melanin production. The effect of QNTs to inhibit melanin formation in B16 melanoma cells was screened in the presence of α-MSH. In defining the mechanism of activity, the effects on tyrosinase activity, on tyrosinase synthesis and on the depigmentation of melanin were evaluated. QNTs did not affect the catalytic activity of tyrosinase, but rather acted as an inhibitor of tyrosinase synthesis.

Original languageEnglish (US)
Pages (from-to)1555-1562
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number4
DOIs
StatePublished - Feb 15 2010

Bibliographical note

Funding Information:
This research was financially supported by a grant ( R01-2007-000-20099-0 ) from the National Research Foundation of Korea .

Keywords

  • 3,4-Dihydroquinazolines
  • Depigmentation
  • Tyrosinase
  • α-Melanocyte stimulating hormone

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