Cinnabaramides A-G: Analogues of Lactacystin and Salinosporamide from a Terrestrial Streptomycete
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- 作者：Marc Stadler ; Jens Bitzer ; Anke Mayer-Bartschmid ; Hartwig Mü ; ller ; Jordi Benet-Buchholz ; Florian Gantner ; Hans-Volker Tichy ; Peter Reinemer ; Kevin B. Bacon
- 刊名：Journal of Natural Products
- 出版年：2007
- 出版时间：February 2007
- 年：2007
- 卷：70
- 期：2
- 页码：246 - 252
- 全文大小：368K
- 年卷期：v.70,no.2(February 2007)
- ISSN：1520-6025
文摘
The cinnabaramides A-G (1-7) were isolated from a terrestrial strain of Streptomyces as potent and selective inhibitorsof the human 20S proteasome. Their chemical and biological properties resemble those of salinosporamide A, a recentlyidentified lead compound from an obligate marine actinomycete, which is currently under development as an anticanceragent. Cinnabaramides F and G (6, 7) combine essential structural features of salinosporamide A and lactacystin andshow about equal potency in vitro, with IC50 values in the 1 nM range. The properties and phylogenetic position of theproducer organism, the production and isolation of compounds 1-7, their structure elucidation by MS and NMR, andtheir biological activities are reported. Additionally, an X-ray crystal structure was obtained from cinnabaramide A (1).