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

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

  • Bioorg Med Chem Lett. 2017 Aug 1;27(15):3374-3377. doi: 10.1016/j.bmcl.2017.06.011.
Hyeju Jo 1 Minho Choi 1 Jaeuk Sim 1 Mayavan Viji 1 Siyuan Li 1 Young Hee Lee 1 Youngsoo Kim 1 Seung-Yong Seo 2 Yuanyuan Zhou 3 Kiho Lee 3 Wun-Jae Kim 4 Jin Tae Hong 1 Heesoon Lee 1 Jae-Kyung Jung 5
Affiliations

Affiliations

  • 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.

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