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Title: Chemistry and biology of ophiobolin A and its congeners
Authors: Kornienko, A. V.
Корниенко, А. В.
Keywords: Anticancer activity;Apoptosis resistance;Glioblastoma;Ophiobolin A;Sesterterpenes
Issue Date: 2019
Publisher: Elsevier Ltd
Citation: Masi, M., Dasari, R., Evidente, A., Mathieu, V., Kornienko, A. Chemistry and biology of ophiobolin A and its congeners // Bioorganic and Medicinal Chemistry Letters. - 2019
Series/Report no.: Bioorganic and Medicinal Chemistry Letters
Abstract: Ophiobolin A is a fungal secondary metabolite that was found to have significant activity against apoptosis-resistant glioblastoma cells through the induction of a non-apoptotic cell death, offering an innovative strategy to combat this aggressive cancer. The current article aims to make the bridge between the anti-cancer effects of ophiobolin A and its unique reaction with primary amines and suggests that pyrrolylation of lysine residues on its intracellular target protein(s) and/or phosphatidylethanolamine lipid is responsible for its biological effects. The article also discusses chemical derivatization of ophiobolin A to establish first synthetically generated structure-activity relationship. Finally, the reported total synthesis efforts toward the ophiobolin class of sesterterpenes are discussed and identified as a fertile area for improvement in pursuit of these molecules as anticancer agents
Appears in Collections:Статьи, проиндексированные в SCOPUS, WOS

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