The development of desired multitarget agents may provide an attractive and cost-effective complement or alternative to drug combinations. BET and HDAC, as important epigenetic modulators, are both attractive targets in drug discovery and development. Considering the fact that BET and HDAC inhibitors exert a synergistic effect on cellular processes in cancer cells, the design of dual BET/HDAC inhibitors may be a rational strategy to improve the efficacy of their single-target drugs for tumor treatment. In current review, we depict the development of dual BET/HDAC inhibitors and particularly highlight their SARs, binding modes and biological functions with the aim to facilitate rational design and develop more dual BET/HDAC inhibitors.

期望的多靶点药物的开发可以提供有吸引力且具有成本效益的补充剂或替代药物组合。BET和HDAC作为重要的表观遗传调节剂，在药物发现和开发中都是有吸引力的靶标。考虑到BET和HDAC抑制剂对癌细胞的细胞过程具有协同作用这一事实，双重BET / HDAC抑制剂的设计可能是提高其单靶标药物治疗肿瘤疗效的合理策略。在当前的审查中，我们描绘了双重BET / HDAC抑制剂的发展，并特别强调了它们的SAR，结合模式和生物学功能，目的是促进合理设计并开发更多的双重BET / HDAC抑制剂。