Method for preparing largazole analogs and uses thereof
申请人:Williams Robert M.
公开号:US20100029731A1
公开(公告)日:2010-02-04
Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.
Synthesis and Histone Deacetylase Inhibitory Activity of Largazole Analogs: Alteration of the Zinc-Binding Domain and Macrocyclic Scaffold
作者:Albert A. Bowers、Nathan West、Tenaya L. Newkirk、Annie E. Troutman-Youngman、Stuart L. Schreiber、Olaf Wiest、James E. Bradner、Robert M. Williams
DOI:10.1021/ol900078k
日期:2009.3.19
Fourteen analogs of the marine natural product largazole have been prepared and assayed against histone deacetylases (HDACs) 1, 2, 3, and 6. Olefin cross-metathesis was used to efficiently access six variants of the side-chain zinc-binding domain, while adaptation of our previously reported modular synthesis allowed probing of the macrocyclic cap group.
Method for Preparing Largazole Analogs and Uses Thereof
申请人:Williams Robert M.
公开号:US20120264794A1
公开(公告)日:2012-10-18
Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.