Histone deacetylases (HDACs) are epigenetic regulators of chromatin condensation and decondensation and exert effects on the proliferation and spread of cancer. Thus, HDAC enzymes are promising drug targets for the treatment of cancer. Some HDAC inhibitors such as the hydroxamic acid derivatives vorinostat or panobinostat were already approved for the treatment of hematologic cancer diseases, and are under intensive investigation for their use in solid tumors. But there are also drawbacks of the clinical application of HDAC inhibitors like intrinsic or acquired drug resistance and, thus, new HDAC inhibitors with improved activities are sought for. Kinase inhibitors are very promising anticancer drugs and often showed synergistic anticancer effects in combination with HDAC inhibitors. Several hybrid molecules with HDAC and kinase inhibitory structural motifs were disclosed with even improved anticancer activities when compared with co-application of HDAC and receptor tyrosine kinase inhibitors. Chimeric inhibitors with HDAC inhibitory activities exert a rapidly growing field of research and only in this year several new dual HDAC/kinase inhibitors were disclosed. This review briefly summarizes the status and future perspective of the most advanced and promising dual HDAC/kinase inhibitors and their potential as anticancer drug candidates.

组蛋白去乙酰化酶 (HDAC) 是染色质浓缩和去浓缩的表观遗传调节剂，对癌症的增殖和扩散产生影响。因此，HDAC酶是治疗癌症的有希望的药物靶标。一些 HDAC 抑制剂，如异羟肟酸衍生物伏立诺他或帕比司他已被批准用于治疗血液系统癌症疾病，并且正在对它们在实体瘤中的应用进行深入研究。但HDAC抑制剂的临床应用也存在内在或获得性耐药性等缺点，因此寻求具有改善活性的新型HDAC抑制剂。激酶抑制剂是非常有前景的抗癌药物，并且经常与 HDAC 抑制剂组合显示出协同抗癌作用。与 HDAC 和受体酪氨酸激酶抑制剂的共同应用相比，公开了几种具有 HDAC 和激酶抑制结构基序的杂合分子具有甚至提高的抗癌活性。具有 HDAC 抑制活性的嵌合抑制剂是一个快速发展的研究领域，仅在今年才公开了几种新的 HDAC/激酶双重抑制剂。本综述简要总结了最先进和最有前途的双重 HDAC/激酶抑制剂的现状和未来前景及其作为抗癌候选药物的潜力。具有 HDAC 抑制活性的嵌合抑制剂是一个快速发展的研究领域，仅在今年才公开了几种新的 HDAC/激酶双重抑制剂。本综述简要总结了最先进和最有前途的双重 HDAC/激酶抑制剂的现状和未来前景及其作为抗癌候选药物的潜力。具有 HDAC 抑制活性的嵌合抑制剂是一个快速发展的研究领域，仅在今年才公开了几种新的 HDAC/激酶双重抑制剂。本综述简要总结了最先进和最有前途的双重 HDAC/激酶抑制剂的现状和未来前景及其作为抗癌候选药物的潜力。