Discovery of a biologically active thiostrepton fragment.

Nicolaou, K C; Zak, Mark; Rahimipour, Shai; Estrada, Anthony A; Lee, Sang Hyup; O'Brate, Aurora; Giannakakou, Paraskevi; Ghadiri, M Reza

Nicolaou, K C; Zak, Mark; Rahimipour, Shai; Estrada, Anthony A; Lee, Sang Hyup; O'Brate, Aurora; Giannakakou, Paraskevi; Ghadiri, M Reza.

Afiliación

Nicolaou KC; Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California 92037, USA. kcn@scripps.edu

J Am Chem Soc ; 127(43): 15042-4, 2005 Nov 02.

Article en En | MEDLINE | ID: mdl-16248640

ABSTRACT

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.

Asunto(s)

Enterococcus faecalis/efectos de los fármacos; Escherichia coli/efectos de los fármacos; Plasmodium falciparum/efectos de los fármacos; Staphylococcus/efectos de los fármacos; Tioestreptona/farmacología; Animales; Antibacterianos/farmacología; Humanos; Modelos Químicos; Péptidos/farmacología; Tioestreptona/síntesis química; Tioestreptona/metabolismo

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Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Plasmodium falciparum / Staphylococcus / Tioestreptona / Enterococcus faecalis / Escherichia coli Límite: Animals / Humans Idioma: En Revista: J Am Chem Soc Año: 2005 Tipo del documento: Article País de afiliación: Estados Unidos

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