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, M. Reza Ghadiri

Research output: Contribution to journalArticlepeer-review

60 Scopus citations


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.

Original languageEnglish
Pages (from-to)15042-15044
Number of pages3
JournalJournal of the American Chemical Society
Issue number43
StatePublished - 2 Nov 2005


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