基于组蛋白去乙酰化酶靶点的羟肟酸类化合物及其抗肿瘤活性研究进展

Research Progress in Hydroxamic Acids Based on Histone Deacetylases Targets and Their Antitumor Activities

组蛋白去乙酰化酶(HDACs)是肿瘤治疗的靶点之一,组蛋白去乙酰化酶抑制剂(HDACi)可通过包括抑制肿瘤细胞活力、迁移、侵袭、血管生成、增殖、DNA修复和诱导细胞凋亡等多种机制发挥抗肿瘤作用。本文对近年来以HDACs为单靶点和多靶点的羟肟酸类衍生物的合成及其抗肿瘤活性进行综述,并对此方面的发展趋势、应用前景进行展望。

Tumor therapy includes histone deacetylases(HDACs)as one of its targets.Through a variety of ways,histone deacetylase inhibitors(HDACi)are significant in their anti-tumor performance.It involves the stimulation of apoptosis,DNA repair,angiogenesis,invasion,migration,and viability of tumor cells.This review examined the synthesis and antitumor activity of derivatives of hydroxamic acid that had HDACs as single and multi-targets in recent years.Meanwhile prospects were made regarding the trend of development and potential applications in this area.