苯并咪唑
对接(动物)
化学
体外
细胞周期蛋白依赖激酶
伊马替尼
细胞培养
生物活性
细胞周期蛋白依赖激酶2
激酶
癌细胞
药理学
组合化学
生物化学
立体化学
癌症
癌症研究
细胞
生物
蛋白激酶A
细胞周期
医学
有机化学
护理部
遗传学
髓系白血病
作者
Rania H. Abd El‐Hameed,Samar S. Fatahala,Amira I. Sayed
出处
期刊:Medicinal Chemistry
日期:2021-03-05
卷期号:18 (2): 238-248
被引量:10
标识
DOI:10.2174/1573406417666210304100830
摘要
Thiobezimidazoles reveal various pharmacological activities due to similarities with many natural and synthetic molecules; they can easily interact with biomolecules of living systems.A series of substituted 2-thiobezimidazoles have been synthesized. Twelve final compounds were screened for in vitro anti-cancer activities against sixty different cell lines.The spectral data of the synthesized compounds were characterized. A docking study for active anticancer compounds and CDK2/CyclinA2 Kinase assay against standard reference; Imatinib, were performed.Two compounds (3c&3l) from the examined series revealed effective antitumor activity in vitro against two-cancer cell lines (Colon Cancer (HCT-116) and Renal Cancer (TK-10). The docking study of synthesized molecules discovered a requisite binding pose in the CDK-ATP binding pocket .3c &3l were promoted in the CDK2/CyclinA2 Kinase assay against standard reference Imatinib.Against all tested compounds; two compounds 3c &3l were found active against two types of cell-lines.
科研通智能强力驱动
Strongly Powered by AbleSci AI