Development of a second generation of inhibitors of microsomal prostaglandin E synthase 1 expression bearing the γ-hydroxybutenolide scaffold

M Aquino, MD Guerrero, I Bruno, MC Terencio…

文献索引：Aquino, Maurizio; Guerrero, Maria D.; Bruno, Ines; Terencio, Maria C.; Paya, Miguel; Riccio, Raffaele Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 19 p. 9056 - 9064

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被引用次数: 16

摘要

Petrosaspongiolide M (PM, 1), a marine sesterterpene metabolite bearing the γ- hydroxybutenolide scaffold and displaying a potent inhibitory activity toward PLA2 enzyme, was selected by us as an attractive target in order to explore its mechanism of action at molecular level. In the course of our investigations we decided to synthetically modify the parent compound to clarify the structural determinants responsible for the activity; in fact, ...