Discovery of a Biologically Active Thiostrepton Fragment

K. C. Nicolaou,* Mark Zak, Shai Rahimipour, Anthony A. Estrada, Sang Hyup Lee, Aurora O'Brate,† Paraskevi Giannakakou,† and M. Reza Ghadiri
Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, and Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, California 92093
J. Am. Chem. Soc., 2005, 127 (43), pp 15042–15044
DOI: 10.1021/ja0552803
Publication Date (Web): October 6, 2005
Copyright © 2005 American Chemical Society
*

In papers with more than one author, the asterisk indicates the name of the author to whom inquiries about the paper should be addressed.

,
†

 Winship Cancer Institute, Emory University School of Medicine.

, kcn@scripps.edu

Abstract

Abstract Image

Design, synthesis, and biological evaluation of several domains of the thiopeptide antibiotic thiostrepton led to the discovery of a biologically active fragment. The biological properties of this novel small organic molecule include antibiotic activity against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VREF) bacterial strains, as well as cytotoxic action against a number of cancer cell lines.

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History

  • Published In Issue November 02, 2005
  • Received August 3, 2005

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