一系列强效和选择性酮类组蛋白脱乙酰酶抑制剂的优化
Optimization of a series of potent and selective ketone histone deacetylase inhibitors.
作者信息
Pescatore Giovanna, Kinzel Olaf, Attenni Barbara, Cecchetti Ottavia, Fiore Fabrizio, Fonsi Massimiliano, Rowley Michael, Schultz-Fademrecht Carsten, Serafini Sergio, Steinkühler Christian, Jones Philip
机构信息
IRBM/Merck Research Laboratories, Via Pontina km 30,600, 00040 Pomezia, Italy.
出版信息
Bioorg Med Chem Lett. 2008 Oct 15;18(20):5528-32. doi: 10.1016/j.bmcl.2008.09.003. Epub 2008 Sep 6.
Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy and the first generation HDAC inhibitors are currently in the clinic. Herein we describe the optimization of a series of ketone small molecule HDAC inhibitors leading to potent and selective class I HDAC inhibitors with good dog PK.
组蛋白去乙酰化酶（HDAC）抑制剂为癌症治疗提供了一种有前景的策略，第一代HDAC抑制剂目前正在临床试验中。在此，我们描述了一系列酮类小分子HDAC抑制剂的优化过程，这些优化产生了具有良好犬类药代动力学性质的强效且选择性的I类HDAC抑制剂。
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