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  • Title: Efficient synthesis and structure-activity relationship of honokiol, a neurotrophic biphenyl-type neolignan.
    Author: Esumi T, Makado G, Zhai H, Shimizu Y, Mitsumoto Y, Fukuyama Y.
    Journal: Bioorg Med Chem Lett; 2004 May 17; 14(10):2621-5. PubMed ID: 15109665.
    Abstract:
    Honokiol, a biphenyl-type neolignan, which shows the remarkable neurotrophic effect in primary cultured rat cortical neurons, has been effectively synthesized in 21% yield over 14 steps starting from 5-bromosalicylic acid and p-hydroxybenzoic acid by utilizing Pd-catalyzed Suzuki-Miyaura coupling reaction as a key step. Additionally, the structure-activity relationship between neurite outgrowth-promoting activity and its O-methylated and/or its hydrogenated analogues was examined in the primary cultures of fetal rat cortical neurons, suggesting that 5-allyl and 4'-hydroxyl groups are essential for affecting the neurotrophic activity of honokiol.
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