Geng Aixin, Cui Hao, Zhang Liyuan, Chen Xin, Li Hongmei, Lu Tao, Zhu Yong
Department of Organic Chemistry, School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China.
Department of Organic Chemistry, School of Science, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China; Shanxi Key Laboratory of Natural Products & Chemical Biology, College of Science, Northwest A&F University, Yangling 712100, China.
Bioorg Med Chem Lett. 2019 Jul 1;29(13):1605-1608. doi: 10.1016/j.bmcl.2019.04.047. Epub 2019 Apr 29.
Histone deacetylase (HDAC) inhibitors as an important epigenetic therapeutic strategy affect signaling networks and act synergistically with kinase inhibitors for the treatment of cancer. Herein we presented a series of novel phenoxybenzamide analogues with inhibition of Raf and HDAC. Among them, compound 10e showed potent antiproliferative activities against Hepg2 and MDA-MB-468 in cellular assays. This work may lay the foundation for developing novel dual Raf/HDAC inhibitors as potential anticancer therapeutics.
组蛋白去乙酰化酶（HDAC）抑制剂作为一种重要的表观遗传治疗策略，可影响信号网络，并与激酶抑制剂协同作用以治疗癌症。在此，我们展示了一系列具有抑制Raf和HDAC作用的新型苯氧基苯甲酰胺类似物。其中，化合物10e在细胞实验中对Hepg2和MDA-MB-468显示出强大的抗增殖活性。这项工作可能为开发新型双Raf/HDAC抑制剂作为潜在的抗癌治疗药物奠定基础。
