Histone deacetylases (HDACs) exhibit increased expression in cancer and promote oncogenesis via the acetylation of or interactions with key transcriptional regulators. HDAC inhibitors (HDACis) decrease HDAC activity to selectively inhibit the occurrence and development of tumors. Our study screened and obtained a new HDACi structure. In vitro experiments have showed that among the leads, Z31216525 significantly inhibited the proliferation and induced the apoptosis of epithelial ovarian cancer (EOC) cells. In vivo experiments demonstrated that compared to the control, Z31216525 significantly inhibited tumor growth and showed very low toxicity. Further mechanistic studies revealed that Z31216525 may exert an antitumor effect by inhibiting the expression of the c-Myc gene. Collectively, our studies identified a novel HDACi that is expected to become a new potential therapeutic drug for EOC and has important value for the design of new HDACi structures.

中文翻译：

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发现一种在体内和体外抑制卵巢癌细胞增殖的新型 HDACi 结构

组蛋白去乙酰化酶 (HDAC) 在癌症中表现出增加的表达，并通过乙酰化或与关键转录调节因子的相互作用促进肿瘤发生。HDAC抑制剂（HDACis）降低HDAC活性以选择性地抑制肿瘤的发生和发展。我们的研究筛选并获得了新的 HDACi 结构。体外实验表明，在这些引线中，Z31216525显着抑制卵巢上皮癌（EOC）细胞的增殖并诱导其凋亡。体内实验表明，与对照相比，Z31216525 显着抑制肿瘤生长并表现出非常低的毒性。进一步的机制研究表明，Z31216525 可能通过抑制 c-Myc 基因的表达发挥抗肿瘤作用。总的来说，我们的研究确定了一种新的 HDACi，有望成为 EOC 的一种新的潜在治疗药物，对设计新的 HDACi 结构具有重要价值。