Salicylaldehyde Benzoylhydrazones with Anticancer Activity and Selectivity: Design, Synthesis, and In Vitro Evaluation

被引:0
|
作者
Nikolova-Mladenova, Boryana [1 ]
Mihaylova, Rositsa [2 ]
Atanasova, Mariyana [1 ]
Zhivkova, Zvetanka [1 ]
Doytchinova, Irini [1 ]
机构
[1] Med Univ Sofia, Fac Pharm, Dept Chem, 2 Dunav Str, Sofia 1000, Bulgaria
[2] Med Univ Sofia, Fac Pharm, Dept Pharmacol Pharmacotherapy & Toxicol, 2 Dunav Str, Sofia 1000, Bulgaria
来源
MOLECULES | 2025年 / 30卷 / 05期
关键词
salicylaldehyde; hydrazones; methoxy group; antileukemic activity; selectivity; CHRONIC MYELOID-LEUKEMIA; DRUG-BINDING; QUANTITATIVE STRUCTURE; CRYSTAL-STRUCTURES; LIGANDS SYNTHESIS; CANCER; COMPLEXES; SIMULATION; PREDICTION; INHIBITOR;
D O I
10.3390/molecules30051015
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
Dimethoxy derivatives of salicylaldehyde benzoylhydrazone containing a methoxy group on both aromatic rings were designed and synthesized. The compounds were obtained in high yields, and their structures were confirmed by elemental analysis and various spectral techniques. In vitro evaluation of dimethoxy hydrazones demonstrated potent activity against the leukemic cell lines at low micro- and nanomolar concentrations. Remarkably, two dimethoxy analogs showed exceptional antileukemic selectivity, with no toxicity observed in normal human embryonic kidney HEK-293 cells. In silico modeling identified likely interactions with the target, human cAbl kinase, and suggested a possible mechanism for their antileukemic activity.
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页数:18
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