Nobiletin metabolites: Synthesis and inhibitory activity against matrix metalloproteinase-9 production

作者：Oshitari Tetsuta^*; Okuyama Yuji; Miyata Yoshiki; Kosano Hiroshi; Takahashi Hideyo; Natsugari Hideaki

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(15): 4540-4544.

DOI：10.1016/j.bmcl.2011.05.121

• Nobiletin
• Polymethoxyflavone
• Ulmann reaction
• Baker-Venkataraman rearrangement
• Matrix metalloproteinase-9

A divergent synthesis of nobiletin metabolites was developed through highly oxygenated acetophenone derivative. We used commercially available methyl 3,4,5-trimethoxybenzoate as a starting material for concise preparation of the key intermediate, 2'-hydroxy-3',4',5',6'-tetramethoxyacetophenone (I). These metabolites showed strong inhibitory activity against matrix metalloproteinase-9 production in human lens epithelial cells.

• 出版日期2011-8-1