Synthesis, Biological Evaluation, and Molecular Docking Study of New Pyrazoline-Based Compounds

被引:0
|
作者
Al-halki, A. A. [1 ]
Al-amshany, Z. M. [1 ]
Tashkandi, N. Y. [1 ]
El-shishtawy, R. M. [1 ,2 ]
机构
[1] King Abdulaziz Univ, Fac Sci, Chem Dept, Jeddah 21551, Saudi Arabia
[2] Natl Res Ctr, Text Res Div, Dyeing Printing & Text Auxiliaries Dept, Cairo 12622, Egypt
关键词
chalcones; pyrazoline-thiazolinone; pyrazoline-thiazole; antimicrobial activity; molecular docking; VEGFR-2; kinase; DERIVATIVES; ANTICANCER; THIAZOLE; RESISTANCE; INHIBITORS; CHALCONES; DESIGN; POTENT; KINASE;
D O I
10.1134/S1070363223100158
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The current study represents the synthesis and characterization of new pyrazoline, pyrazoline-thiazolinone, and pyrazoline-thiazole-based derivatives, using 1-(4-aminophenyl)-3-substituted phenylprop-2-en-1-ones as the key intermediate precursors. In order to decrease the reaction times and boost the yields of the target compounds, microwave irradiation at 80 degrees C was utilized to synthesize the pyrazoline and thiazolinone derivatives. All the new analogues were subjected to antimicrobial evaluation against different gram-positive, gram-negative bacteria and the pathogenic yeast Candida albicans. In addition, the docking simulation study of the thiazolinone and the thiazole derivatives against VEGFR-2 kinase was carried out in comparison with the ligand sorafenib. The results confirmed that the pyrazoline-thiazole compounds represented good stability and fixation within the active site of VEGFR-2 and could be considered basic scaffolds for the discovery of new promising anticancer compounds.
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页码:2608 / 2620
页数:13
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