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Bioorg Med Chem Lett. 2017 Aug 1;27(15):3374-3377. doi: 10.1016/j.bmcl.2017.06.011. Epub 2017 Jun 3.

Synthesis and biological evaluation of caffeic acid derivatives as potent inhibitors of α-MSH-stimulated melanogenesis.

Author information

1
College of Pharmacy and Medicinal Research Center (MRC), Chungbuk National University, Cheongju 28160, Republic of Korea.
2
College of Pharmacy and Gachon Institute of Pharmaceutical Sciences, Gachon University, Incheon 21936, Republic of Korea. Electronic address: syseo@gachon.ac.kr.
3
College of Pharmacy, Korea University, Sejong 30019, Republic of Korea.
4
College of Medicines, Chungbuk National University, Cheongju 28644, Republic of Korea.
5
College of Pharmacy and Medicinal Research Center (MRC), Chungbuk National University, Cheongju 28160, Republic of Korea. Electronic address: orgjkjung@chungbuk.ac.kr.

Abstract

We have disclosed our effort to develop caffeic acid derivatives as potent and non-toxic inhibitors of α-MSH-stimulated melanogenesis to treat pigmentation disorders and skin medication including a cosmetic skin-whitening agent. The SAR studies revealed that cyclohexyl ester and secondary amide derivatives of caffeic acid showed significant inhibitory activities.

KEYWORDS:

Caffeamide; Caffeic acid; Melanogenesis; Skin whitening; α-MSH

PMID:
28619537
DOI:
10.1016/j.bmcl.2017.06.011
[Indexed for MEDLINE]

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