Synthesis and bioactivity of novel isoxazole chalcone derivatives on tyrosinase and melanin synthesis in murine B16 cells for the treatment of vitiligo
文献类型：期刊论文
| 作者 | 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)
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
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| 出版日期 | 2016 |
| 卷号 | 24期号:21页码:5440-5448 |
| 关键词 | Chalcone Tyrosinase Melanin synthesis SAR Vitiligo |
| 通讯作者 | Aisa, HA |
| 英文摘要 | 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. |
| 收录类别 | SCI |
| WOS记录号 | WOS:000386990200046 |
| 源URL | [http://ir.xjipc.cas.cn/handle/365002/4628]  |
| 专题 | 新疆理化技术研究所_省部共建新疆特有药用资源利用重点实验室 新疆理化技术研究所_资源化学研究室 |
| 作者单位 | 1.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 |
| 推荐引用方式 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. |
入库方式： OAI收割
来源：新疆理化技术研究所
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