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

doi:10.1021/ja0552803

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

Department of Chemistry

Emory University

Research output: Contribution to journal › Article › peer-review

64 Scopus citations

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.

Original language	English
Pages (from-to)	15042-15044
Number of pages	3
Journal	Journal of the American Chemical Society
Volume	127
Issue number	43
DOIs	https://doi.org/10.1021/ja0552803
State	Published - 2 Nov 2005

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10.1021/ja0552803

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AU - O'Brate, Aurora

AU - Giannakakou, Paraskevi

AU - Ghadiri, M. Reza

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AB - 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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Discovery of a biologically active thiostrepton fragment

Abstract

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