Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors

被引：2
|
作者：
Abdullah, Omeima [1 ]
机构：
[1] Umm Al Qura Univ, Coll Pharm, Mecca 21955, Saudi Arabia
来源：
MOLECULES | 2021年 / 26卷 / 18期
关键词：
cancer; Aurora-A; kinase; triazole;
D O I：
10.3390/molecules26185678
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 IC(50)s in the low to submicromolar range.
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页数：5
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