Preparation and biological evaluation of key fragments and open analogs of scleritodermin A

The synthesis of key fragments of scleritodermin A, their assembly, and their biological evaluation as cytotoxic and anthelmintic were performed. Highlights of the synthetic route include formation of the α-ketoamide linkage and use of stereocontrolled reactions. Open analogs of this natural product were obtained using a convergent strategy.

Graphical abstractThe synthesis of different key fragments of scleritodermin A, their assembly to obtain open analogs, and biological evaluation of the obtained products as cytotoxic and anthelmintic were performed.Figure optionsDownload full-size imageDownload as PowerPoint slide