Haidar S, Jabbour M, Al-Khayat M A, Aichele D, Jose J
Pharmazie. 2018 Apr 2;73(4):191-195. doi: 10.1681/ph.2018.7971.
Protein kinase CK2 is a potential drug target for many diseases including cancer, inflammatory disorders, Alzheimer's disease, Parkinson's disease and viral infections. Significant efforts have been made for the discovery of potent inhibitors of this enzyme. Herein, we report on the synthesis, characterization, and biological evaluation of novel flavonoid compounds as CK2 inhibitors. The tested compounds were 2 (4`-hydroxynaphthyl) chromen-4-one which is a naphthyl backbone flavonoid with an IC50 value of 0.45±0.059 μM and 2(4-hydroxyphenyl)-4H-chromen-4-one a phenyl based derivative with an IC50 value of 0.33±0.048 μM. Cell viability was tested using MCF-7 cells. Both compounds were able to reduce the cell viability around 50 % in concentration of 100 μM after 48 h. Molecular modeling studies were performed to understand the binding mode of both compounds.
蛋白激酶CK2是包括癌症、炎症性疾病、阿尔茨海默病、帕金森病和病毒感染在内的多种疾病的潜在药物靶点。人们为发现该酶的有效抑制剂付出了巨大努力。在此，我们报告了新型黄酮类化合物作为CK2抑制剂的合成、表征及生物学评价。测试的化合物为2-(4`-羟基萘基)色原酮-4-酮，它是一种萘基骨架黄酮，IC50值为0.45±0.059 μM；以及2-(4-羟基苯基)-4H-色原酮-4-酮，一种苯基衍生物，IC50值为0.33±0.048 μM。使用MCF-7细胞测试细胞活力。在100 μM浓度下处理48小时后，两种化合物均能使细胞活力降低约50%。进行了分子模拟研究以了解两种化合物的结合模式。
