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

doi:10.1016/j.bmc.2010.01.005

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

The Hormel Institute

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	1555-1562
Number of pages	8
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	4
DOIs	https://doi.org/10.1016/j.bmc.2010.01.005
State	Published - 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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmc.2010.01.005

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

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.",

keywords = "3,4-Dihydroquinazolines, Depigmentation, Tyrosinase, α-Melanocyte stimulating hormone",

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

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

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doi = "10.1016/j.bmc.2010.01.005",

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T1 - Evaluation of 3,4-dihydroquinazoline-2(1H)-thiones as inhibitors of α-MSH-induced melanin production in melanoma B16 cells

AU - Thanigaimalai, P.

AU - Lee, Ki Cheul

AU - Bang, Seong Cheol

AU - Lee, Jee Hyun

AU - Yun, Cheong Yong

AU - Roh, Eunmiri

AU - Hwang, Bang Yeon

AU - Kim, Youngsoo

AU - Jung, Sang Hun

N1 - Funding Information: This research was financially supported by a grant ( R01-2007-000-20099-0 ) from the National Research Foundation of Korea .

PY - 2010/2/15

Y1 - 2010/2/15

N2 - 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.

AB - 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.

KW - 3,4-Dihydroquinazolines

KW - Depigmentation

KW - Tyrosinase

KW - α-Melanocyte stimulating hormone

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JO - Bioorganic and Medicinal Chemistry

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

Abstract

Bibliographical note

Keywords

UN SDGs

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