多模态HDAC抑制剂具有改善的抗癌活性

Title:Multimodal HDAC Inhibitors with Improved Anticancer Activity

Volume: 18 Issue: 1

关键词: 抗癌药物，表观遗传学，组蛋白脱乙酰酶，激酶，DNA靶向，HDAC抑制剂，杂合分子

摘要: Histone deacetylases (HDACs) play a significant role in the proliferation and dissemination of cancer and represent promising epigenetic drug targets. The HDAC inhibitor vorinostat featuring a zinc-binding hydroxamate fragment was already clinically approved. However, HDAC inhibitors containing hydroxamic acids are often hampered by acquired or intrinsic drug resistance and may lead to enhanced tumor aggressiveness. In order to overcome these drawbacks of hydroxamate HDAC inhibitors, a series of multimodal derivatives of this compound class, including such with different zinc-binding groups, was recently developed and showed promising anticancer activity. This review provides an overview of the chemistry and pleiotropic anticancer modes of action of these conceptually new HDAC inhibitors.

Cite this article as:

Multimodal HDAC Inhibitors with Improved Anticancer Activity, Current Cancer Drug Targets 2018; 18 (1) . https://dx.doi.org/10.2174/1568009617666170206102613