Synthesis and pharmacological activity of diterpenylnaphthoquinone derivatives

二萜萘醌衍生物的合成及药理活性

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作者:Mariano Walter Pertino, Cristina Theoduloz, Jose Antonio Palenzuela, Maria del Mar Afonso, Erdem Yesilada, Francisco Monsalve, Paulo González, Daniel Droguett, Guillermo Schmeda-Hirschmann

Abstract

New diterpenylquinones, combining a diterpene diacid and a naphthoquinone, were prepared from junicedric acid and lapachol. The new derivatives were assessed as gastroprotective agents by the HCl-EtOH-induced gastric lesions model in mice as well as for basal cytotoxicity on the following human cell lines: Normal lung fibroblasts (MRC-5), gastric epithelial adenocarcinoma (AGS), and hepatocellular carcinoma (Hep G2). Several of the new compounds were significantly active as antiulcer agents and showed selective cytotoxicity against AGS cells.

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