Design and synthesis of histone deacetylase inhibitors: the development of apicidin transition state analogs
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- 作者：Colletti ; Steven L. ; Myers ; Robert W. ; Darkin-Rattray ; Sandra J. ; Schmatz ; Dennis M. ; Fisher ; Michael H. ; et. al.
- 关键词：apicidin ; side chain ; transition state inhibitors ; histone deacetylase
- 刊名：Tetrahedron Letters
- 出版年：2000
- 出版时间：October 7, 2000
- 年：2000
- 卷：41
- 期：41
- 页码：7837-7841
- 全文大小：104 K
文摘
A four step degradation of the C8 ethyl ketone of apicidin provided a route to the C6 aldehyde intermediate and several mechanism-based transition state inhibitors of histone deacetylase. The compounds generated herein delineate the significance of apicidin's side chain, highlighted by the high affinity C8 aldehyde and C8-keto-9,10-epoxide analogs of apicidin.