期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2010, 期 21, 页码 3991-4003出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201000317
关键词
Synthetic methods; Natural products; Biological activity; Metathesis; Inhibitors
资金
- Swiss National Science Foundation [3100A0-115970]
A convergent synthesis of SylA was developed and consists of the synthesis of a fully functionalized macrocycle, which is subsequently coupled with a urea moiety. For cyclization, ring-closing metathesis of a conformationally preorganized precursor was employed. The established synthetic route was then applied to the synthesis of SylA derivatives by using various peptidic side chains for decoration of the SylA macrocycle. The resulting collection of SylA analogues was tested for proteasome inhibition, revealing PEGylated SylA derivatives as the most potent proteasome inhibitors.
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