Aurora-A kinase, a key mitosis regulator, is expressed in a cell cycle-dependent manner and has an essential role in maintaining chromosomal stability and the normal progression of the cell through mitosis. Aurora-A kinase is overexpressed in many malignant solid tumors, such as breast, ovarian, colon, and pancreatic cancers. Thus, inhibiting Aurora-A kinase activity is a promising approach for cancer treatment. Here, new triazole derivatives were designed as bioisosteric analogues of the known inhibitor JNJ-7706621. The new compounds showed interesting inhibitory activity against Aurora-A kinase, as attested by IC₅₀s in the low to submicromolar range.

中文翻译：

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作为 Aurora-A 激酶抑制剂的新型三唑衍生物的设计、合成和生化评价

Aurora-A 激酶是一种关键的有丝分裂调节因子，以细胞周期依赖性方式表达，在维持染色体稳定性和细胞通过有丝分裂的正常进程中具有重要作用。Aurora-A 激酶在许多恶性实体肿瘤中过度表达，例如乳腺癌、卵巢癌、结肠癌和胰腺癌。因此，抑制 Aurora-A 激酶活性是一种很有前景的癌症治疗方法。在这里，新的三唑衍生物被设计为已知抑制剂 JNJ-7706621 的生物等排类似物。低至亚微摩尔范围内的IC ₅₀ s证明了新化合物对 Aurora-A 激酶具有有趣的抑制活性。