Discovery of a biologically active thiostrepton fragment
KC Nicolaou, M Zak, S Rahimipour…
Index: Nicolaou; Safina, Brian S.; Zak, Mark; Lee, Sang Hyup; Nevalainen, Marta; Bella, Marco; Estrada, Anthony A.; Funke, Christian; Zecri, Frederic J.; Bulat, Stephan Journal of the American Chemical Society, 2005 , vol. 127, # 31 p. 11159 - 11175
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Citation Number: 55
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.
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