Discovery of a biologically active thiostrepton fragment.
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.
Nicolaou
K C
KC
Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California 92037, USA. kcn@scripps.edu
Zak
Mark
M
Rahimipour
Shai
S
Estrada
Anthony A
AA
Lee
Sang Hyup
SH
O'Brate
Aurora
A
Giannakakou
Paraskevi
P
Ghadiri
M Reza
MR
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*
D000900:Anti-Bacterial Agents; D010455:Peptides; D013883:Thiostrepton