College of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia.
Molecules. 2021 Sep 18;26(18):5678. doi: 10.3390/molecules26185678.
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 ICs in the low to submicromolar range.
极光激酶 A 是一种关键的有丝分裂调节因子，其表达具有细胞周期依赖性，在维持染色体稳定性和细胞有丝分裂的正常进程中起着重要作用。极光激酶 A 在许多恶性实体瘤中过度表达，如乳腺癌、卵巢癌、结肠癌和胰腺癌。因此，抑制极光激酶 A 的活性是癌症治疗的一种有前途的方法。在这里，新的三唑衍生物被设计为已知抑制剂 JNJ-7706621 的生物等排体类似物。新化合物对极光激酶 A 表现出有趣的抑制活性，其 IC 在低至亚微摩尔范围内。
