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Design, Synthesis and Biological Activity of Novel Furocoumarin Derivatives as Stimulators of Melanogenesis and Tyrosinase in B16 Cells

Design, Synthesis and Biological Activity of Novel Furocoumarin Derivatives as Stimulators of Melanogenesis and Tyrosinase in B16 Cells
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摘要 Sixteen novel and four known(4a, 4d, 4e, 4h) amine derivatives of furocoumarin were synthesized, then submitted to evaluation as stimulators of melanogenesis and tyrosinase in B16 murine cells. Among them, five compounds(4g, 4j-4m) showed potent activating effect on both melanogenesis and tyrosinase in vitro compared with positive control(8-MOP), the most widely used drugs for vitiligo in clinic. Noticeably, compotmds 4h and 4j, which contain morpholine and piperazine, were recognized as the most effective stimnlator of melanogenesis and tyrosianse in B16 cells separately. These derivatives may serve as lead compounds for further drug discovery for the treatment of vitiligo. Sixteen novel and four known(4a, 4d, 4e, 4h) amine derivatives of furocoumarin were synthesized, then submitted to evaluation as stimulators of melanogenesis and tyrosinase in B16 murine cells. Among them, five compounds(4g, 4j-4m) showed potent activating effect on both melanogenesis and tyrosinase in vitro compared with positive control(8-MOP), the most widely used drugs for vitiligo in clinic. Noticeably, compotmds 4h and 4j, which contain morpholine and piperazine, were recognized as the most effective stimnlator of melanogenesis and tyrosianse in B16 cells separately. These derivatives may serve as lead compounds for further drug discovery for the treatment of vitiligo.
出处 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2018年第3期408-414,共7页 高等学校化学研究(英文版)
关键词 FUROCOUMARIN AMINE Melanin synthesis TYROSINASE VITILIGO Furocoumarin Amine Melanin synthesis Tyrosinase Vitiligo
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