Towards immunoproteasome-specific inhibitors: An improved synthesis of dihydroeponemycin

被引:13
作者
Ho, A [1 ]
Cyrus, K [1 ]
Kim, KB [1 ]
机构
[1] Univ Kentucky, Coll Pharm, Dept Pharmaceut Sci, Lexington, KY 40536 USA
关键词
immunoproteasome; dihydroeponemycin; phosphonate; Wittig-Horner reaction; Baylis-Hillman reaction;
D O I
10.1002/ejoc.200500437
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Eponemycin, an antitumor and antiangiogenic epoxy ketone natural product, is previously shown to target proteasome for its activity. Although there have been many synthetic approaches developed, practical and efficient synthetic strategy for eponemycin has yet to be accomplished. Here, we report an efficient new route for the preparation of dihydroeponemycin, an active eponemycin derivative. This will aid the design of proteasome inhibitors with novel activity. ((c) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005).
引用
收藏
页码:4829 / 4834
页数:6
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