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

被引:21
作者
Jo, Hyeju [1 ,2 ]
Choi, Minho [1 ,2 ]
Sim, Jaeuk [1 ,2 ]
Viji, Mayavan [1 ,2 ]
Li, Siyuan [1 ,2 ]
Lee, Young Hee [1 ,2 ]
Kim, Youngsoo [1 ,2 ]
Seo, Seung-Yong [3 ,4 ]
Zhou, Yuanyuan [5 ]
Lee, Kiho [5 ]
Kim, Wun-Jae [6 ]
Hong, Jin Tae [1 ,2 ]
Lee, Heesoon [1 ,2 ]
Jung, Jae-Kyung [1 ,2 ]
机构
[1] Chungbuk Natl Univ, Coll Pharm, Cheongju 28160, South Korea
[2] Chungbuk Natl Univ, Med Res Ctr, Cheongju 28160, South Korea
[3] Gachon Univ, Coll Pharm, Incheon 21936, South Korea
[4] Gachon Univ, Gachon Inst Pharmaceut Sci, Incheon 21936, South Korea
[5] Korea Univ, Coll Pharm, Sejong 30019, South Korea
[6] Chungbuk Natl Univ, Coll Med, Cheongju 28644, South Korea
基金
新加坡国家研究基金会;
关键词
Caffeic acid; Melanogenesis; alpha-MSH; Caffeamide; Skin whitening; B16; MELANOMA-CELLS; TYROSINASE INHIBITORS; DOWN-REGULATION; SIGNALING PATHWAYS; SKIN PIGMENTATION; AGENTS; MELANOCYTES; DISCOVERY; ESTER;
D O I
10.1016/j.bmcl.2017.06.011
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We have disclosed our effort to develop caffeic acid derivatives as potent and non-toxic inhibitors of alpha-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. (C) 2017 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3374 / 3377
页数:4
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