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Medicinal Chemistry

ISSN: 2161-0444

Open Access

Hemisynthesis of Anisomycin Derivatives as Antitumor Agents

Abstract

Perrine Six, Jean-François Goossens, William Riquet, Viviane Brel, Emmanuel Fournier, Jean-Philippe Annereau, Anna Kruczynski, Omar Castillo-Aguilera, Patrick Depreux, Christian Bailly and Laurence Goossens

The antibiotic anisomycin, secreted by Streptomyces griseolus, can induce tumor cell death and it displays antimetastatic activity coupled with induction of apoptosis. Herein we report the hemi-synthesis of 16 novel anisomycin derivatives and their biological activity. The protein synthesis inhibition and the effects on cancer cell proliferation and migration were assessed for two series of molecules to determine structure-activity relationships. The secondary amino group of anisomycin is essential to preserve the bioactivity. Although, the natural product is the most active component of the series but an active derivative has been identified

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