Design and synthesis of a vialinin A analog with a potent inhibitory activity of TNF-alpha production and its transformation into a couple of bioprobes

[摘要]：Vialinin A (1) is an extremely potent inhibitor against tumor necrosis factor (TNF)-alpha production in rat basophilic leukemia (RBL-2H3) cells. This Letter describes the design and synthesis of its advanced analog, 50,60-dimethyl-1,1':4'1 ''-terphenyl-2',3',4,4 ''-tetraol (2) with a comparable inhibitory activity (IC50 = 0.02 nM) to that of 1. The synthesis involved double Suzuki-Miyaura coupling as a key step, and required only five steps from commercially available 3,4-dimethylphenol. For identification of the target molecule, fluorescent and biotinylated derivatives of 2 were prepared through a 'click' coupling process. (C) 2012 Elsevier Ltd. All rights reserved.

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