title: Discovery of a biologically active thiostrepton fragment.
abstract: 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.
authors.affiliation: Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California 92037, USA. kcn@scripps.edu
authors.forename: K C
authors.initials: KC
authors.lastname: Nicolaou
authors.forename: Mark
authors.initials: M
authors.lastname: Zak
authors.forename: Shai
authors.initials: S
authors.lastname: Rahimipour
authors.forename: Anthony A
authors.initials: AA
authors.lastname: Estrada
authors.forename: Sang Hyup
authors.initials: SH
authors.lastname: Lee
authors.forename: Aurora
authors.initials: A
authors.lastname: O'Brate
authors.forename: Paraskevi
authors.initials: P
authors.lastname: Giannakakou
authors.forename: M Reza
authors.initials: MR
authors.lastname: Ghadiri
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D013293:Enterococcus faecalis / Q000187:drug effects*; D004926:Escherichia coli / Q000187:drug effects*; D006801:Humans; D008956:Models, Chemical; D010455:Peptides / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects*; D013210:Staphylococcus / Q000187:drug effects*; D013883:Thiostrepton / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D010455:Peptides; D013883:Thiostrepton