期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 25, 期 6, 页码 1451-1455出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201805420
关键词
BCD ring; gedunin; Hsp90p23; limonoids; medicinal chemistry; natural products
资金
- University of Queensland (UQ)
- Australian Research Council [FT110100851, DP130103858]
- Australian Government
D-Ring-seco-limonoids (tetranortriterpenoids), such as gedunin and xylogranin B display anti-cancer activity, acting via inhibition of Hsp90 and/or associated chaperon machinery (e.g., p23). Despite this, these natural products have received relatively little attention, both in terms of an enabling synthetic approach (which would allow access to derivatives), and as a consequence their structure-activity relationship (SAR). Disclosed herein is a generally applicable synthetic route to the BCD ring system of the seco-D-ring double bond containing limonoids. Furthermore, cell based assays revealed the first skeletal fragment that exhibited inhibition of the p23 enzyme at a level which was equipotent to that of gedunin, despite being much less structurally complex.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据