拉戈唑类似物的合成及其组蛋白去乙酰化酶抑制活性：锌结合结构域和大环支架的改变
Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold.
作者信息
Bowers Albert A, West Nathan, Newkirk Tenaya L, Troutman-Youngman Annie E, Schreiber Stuart L, Wiest Olaf, Bradner James E, Williams Robert M
机构信息
Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA.
出版信息
Org Lett. 2009 Mar 19;11(6):1301-4. doi: 10.1021/ol900078k.
Abstract
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.
摘要
已制备了14种海洋天然产物拉戈唑的类似物，并针对组蛋白脱乙酰酶（HDAC）1、2、3和6进行了测定。采用烯烃交叉复分解反应高效合成了六种侧链锌结合结构域变体，同时采用我们之前报道的模块化合成方法对大环封端基团进行了探索。
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J Am Chem Soc. 2009 Mar 4;131(8):2900-5. doi: 10.1021/ja807772w.
2
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