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Synthesis and bioactivity of novel isoxazole chalcone derivatives on tyrosinase and melanin synthesis in murine B16 cells for the treatment of vitiligo
Niu, C (Niu, Chao); Yin, L (Yin, Li); Nie, LF (Nie, Li Fei); Dou, J (Dou, Jun); Zhao, JY (Zhao, Jiang Yu); Li, G (Li, Gen); Aisa, HA (Aisa, Haji Aker)
2016
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
Volume24Issue:21Pages:5440-5448
Abstract

A new series of chalcone derivatives 1-18, bearing isoxazole moieties were designed and synthesized, and biologically evaluated for their activity on mushroom tyrosinase and melanin synthesis in murine B16 cells. The result indicated that most of prepared compounds 1-18 showed potent activating effect on tyrosinase, especially for 1-2, 4, 6-7, 9 and 15. Among them, compounds 2, 4 and 9 demonstrated the best activity with EC50 = 1.3, 2.5 and 3.0 mu mol.L-1 respectively, much better than the positive control 8-methoxypsoralan (8-MOP, EC50 = 14.8 mu mol.L-1); In B16 cells, all the tested compounds exhibited a stronger activity on melanogenesis than 8-MOP (with the value of 115%). It was interesting that derivatives substituted with halogen (1, 2, 4, 5, 7, 9) were generally more potent. Compounds 2 (463%) and 18 (438%) with 3 and 4-fold potency compared with 8-MOP respectively, were recognized as the most promising candidate hits for further pharmacological study of anti-vitiligo.

KeywordChalcone Tyrosinase Melanin Synthesis Sar Vitiligo
DOI10.1016/j.bmc.2016.08.066
Indexed BySCI
WOS IDWOS:000386990200046
Citation statistics
Cited Times:15[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/4628
Collection省部共建新疆特有药用资源利用重点实验室
资源化学研究室
Corresponding AuthorAisa, HA (Aisa, Haji Aker)
Affiliation1.Chinese Acad Sci, Key Lab Plant Resources & Chem Arid Zone, Urumqi 830011, Peoples R China
2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China
Recommended Citation
GB/T 7714
Niu, C ,Yin, L ,Nie, LF ,et al. Synthesis and bioactivity of novel isoxazole chalcone derivatives on tyrosinase and melanin synthesis in murine B16 cells for the treatment of vitiligo[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2016,24(21):5440-5448.
APA Niu, C .,Yin, L .,Nie, LF .,Dou, J .,Zhao, JY .,...&Aisa, HA .(2016).Synthesis and bioactivity of novel isoxazole chalcone derivatives on tyrosinase and melanin synthesis in murine B16 cells for the treatment of vitiligo.BIOORGANIC & MEDICINAL CHEMISTRY,24(21),5440-5448.
MLA Niu, C ,et al."Synthesis and bioactivity of novel isoxazole chalcone derivatives on tyrosinase and melanin synthesis in murine B16 cells for the treatment of vitiligo".BIOORGANIC & MEDICINAL CHEMISTRY 24.21(2016):5440-5448.
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