Cross Jasmine M, Blower Tim R, Gallagher Natalie, Gill Jason H, Rockley Kimberly L, Walton James W
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.
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。
