作为组蛋白去乙酰化酶抑制剂的抗癌钌和铑钢琴凳配合物。
Anticancer Ru and Rh Piano-Stool Complexes that are Histone Deacetylase Inhibitors.
作者信息
Cross Jasmine M, Blower Tim R, Gallagher Natalie, Gill Jason H, Rockley Kimberly L, Walton James W
机构信息
Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, United Kingdom.
School of Biological and Biomedical Sciences, Durham University, South Road, Durham, DH1 3LE, United Kingdom.
出版信息
Chempluschem. 2016 Dec;81(12):1276-1280. doi: 10.1002/cplu.201600413. Epub 2016 Oct 12.
The first examples of Ru and Rh piano-stool complex histone deacetylase (HDAC) inhibitors are presented. The novel complexes have antiproliferative activity against H460 non-small-cell lung carcinoma cells that is comparable to the clinically used HDAC inhibitor suberoylanilide hydroxamic acid (SAHA). Strong evidence for HDAC inhibition as a primary mechanism of action is provided. The complexes reported here represent an important step towards the design of highly active and selective HDAC inhibitors.
首次展示了钌（Ru）和铑（Rh）钢琴凳型配合物组蛋白去乙酰化酶（HDAC）抑制剂的实例。这些新型配合物对H460非小细胞肺癌细胞具有抗增殖活性，与临床使用的HDAC抑制剂辛二酰苯胺异羟肟酸（SAHA）相当。提供了HDAC抑制作为主要作用机制的有力证据。本文报道的配合物代表了设计高活性和选择性HDAC抑制剂的重要一步。
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