Novel benzo[d]imidazole-2(3H)-thiones as potent inhibitors of the α-melanocyte stimulating hormone induced melanogenesis in melanoma B16 cells

Jee Hyun Lee, Pillaiyar Thanigaimalai, Ki Cheul Lee, Seong Cheol Bang, Min Seok Kim, Vinay Kumar Sharma, Cheong Yong Yun, Eunmiri Roh, Youngsoo Kim, Sang Hun Jung

Research output: Contribution to journalArticle

5 Scopus citations

Abstract

In order to determine the optimum size of heterocycle of lead compound 1 (6-methyl-3-phenethyl-3,4-dihydro-1H-quinoline-2-thione; IC50=0.8 μM) for inhibition of melanogenesis, we have synthesized and evaluated some benzimdazole-2(3H)-thiones 5a - e. The preliminary bioassay has shown that the benzimdazole-2(3H)-thione motif of 5 is essential structural unit for their inhibitory activity. Among all thiones 5a - e, the compound 5d strongly inhibited the formation of melanin with IC50 value of 1.3 μM.

Original languageEnglish (US)
Pages (from-to)918-921
Number of pages4
JournalChemical and Pharmaceutical Bulletin
Volume58
Issue number7
DOIs
StatePublished - Jul 2010

Keywords

  • Benzimdazole-2(3H)-thione
  • Inhibitor
  • Melanogenesis

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