新型芳基二硫代烯酮衍生物作为有效的组蛋白去乙酰化酶抑制剂。
New aryldithiolethione derivatives as potent histone deacetylase inhibitors.
机构信息
Sulfidris s.r.l., Viale Gran Sasso 17, 20131 Milan, Italy.
出版信息
Bioorg Med Chem. 2010 Jun 15;18(12):4187-94. doi: 10.1016/j.bmc.2010.05.011. Epub 2010 May 7.
PMID:20576572
Abstract
A series of dithiolethione derivatives was synthesized and the in vitro HDAC inhibitory activity was tested. The most active compounds, 1 and 2, exhibited an IC(50) in nM range with a strong hyperacetylation of histone H4 in A549 cells. The HDAC inhibitory activity comparable to that of SAHA and the inhibition of A549 cell proliferation suggest that these compounds are worthy of further studies as potential anticancer agents.
摘要
合成了一系列二硫代烯酮衍生物，并测试了它们的体外 HDAC 抑制活性。最活跃的化合物 1 和 2，在 A549 细胞中表现出纳摩尔级的 IC（50），并强烈地使组蛋白 H4 乙酰化。其 HDAC 抑制活性可与 SAHA 相媲美，并且能抑制 A549 细胞增殖，表明这些化合物具有作为潜在抗癌剂的进一步研究价值。
Zotero 插件