Synthesis of Simplified Halogenated Chondramide Derivatives with Strong Cytostatic Properties. Issue 12 (9th February 2015)

• Record Type: Journal Article
• Authors: Becker, Dominic; Kazmaier, Uli
• Is Part Of: European journal of organic chemistry. Issue 12(2015)
• Page Start: 2591
• Page End: 2602
• Publication Date: 2015-02-09
• Subjects: Synthetic methods -- Medicinal chemistry -- Anticancer agents -- Cytotoxicity -- Natural products -- Peptides -- Chondramides; Chemistry, Organic -- Periodicals; Organic compounds -- Synthesis -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1002/ejoc.201403577
• Languages: English
• ISSNs: 1434-193X

Abstract

Abstract: Removing the methyl groups and the stereogenic centers from the ω‐hydroxy acid of the chondramides results in a significant drop in the cytotoxicity of these interesting depsipeptides. This effect can be almost compensated for by introduction of a second chlorine atom on the β‐tyrosine moiety of the natural products. These simplified chondramides are much easier accessible than natural chondramides. Abstract : Easily available dichlorinated Chondramide derivatives show high antitumor‐activity towards selected cancer cell lines.