Discovery of a biologically active thiostrepton fragment
Discovery of a biologically active thiostrepton fragment
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DOI：
10.1021/ja0552803
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发表时间：
2005-11-02
影响因子：
15
通讯作者：
Ghadiri, MR
中科院分区：
文献类型：
--
作者：
Nicolaou, KC;Zak, M;Ghadiri, MR
硫肽抗生素thiostrepton的几个结构域的设计、合成和生物学评价导致了生物活性片段的发现。这种新型有机小分子的生物学特性包括对耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素粪肠球菌（VREF）菌株的抗生素活性，以及对许多癌细胞系的细胞毒性作用。
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-resistantStaphylococcus aureus(MRSA) and vancomycin-resistantEnterococcus faecalis(VREF) bacterial strains, as well as cytotoxic action against a number of cancer cell lines.