Design and semisynthesis of novel fredericamycin A derivatives with an improved antitumor profile

We report the design, semisynthesis, and biological activity of a series of fredericamycin (1) derivatives. Within this series compound 1e combines low nanomolar cytotoxic potency in vitro, increased tumor cell line selectivity, and in vivo activity in a human xenograft model.

Starting from natural Fredericamycin A, a series of semisynthetic derivatives was prepared exhibiting increased potency and selectivity in vitro in a human tumor cell line panel.Figure optionsDownload as PowerPoint slide