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

Bioorg Med Chem Lett

Santhera Pharmaceuticals, Im Neuenheimer Feld 518-519, 69120 Heidelberg, Germany.

Published: June 2006

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.

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http://dx.doi.org/10.1016/j.bmcl.2006.03.029DOI Listing

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