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ID: ALA4400555

Journal: Bioorg Med Chem Lett

Title: Structure-activity relationships of trichothecenes against COLO201 cells and Cochliobolus miyabeanus: The role of 12-epoxide and macrocyclic moieties.

Authors: Matsumoto M, Nishiyama M, Maeda H, Tonouchi A, Konno K, Hashimoto M.

Abstract: The novel trichothecene 12-deoxytrichodermin (3) was isolated from the fungus Trichoderma sp. 1212-03, and included with other known natural trichothecenes in a structure-activity relationship investigation against a human colon cancer cell line (COLO201) and filamentous fungus Cochliobolus miyabeanus. This revealed that the 12-epoxide functionality is critical for the cytotoxicity of simple trichothecenes trichodermin (4) and deoxynivalenol (2), while not critical for the cytotoxicity of roridin J (6) and epiisororidin E (8). In contrast, 12-epoxide is essential for the antifungal activity.

CiteXplore: 30797671

DOI: 10.1016/j.bmcl.2019.02.015