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

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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Publication Details

Journal
Molecules
Published
2025-02-22
DOI
https://doi.org/10.3390/molecules30051015
Citations
2
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
1.87
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article

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

Zvetanka Zhivkova, Mariyana Atanasova, Rositsa Mihaylova, Irini Doytchinova et al.
2 citations
Molecules
Synthesis and biological activity
1.87
article

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

Zvetanka Zhivkova, Mariyana Atanasova, Rositsa Mihaylova, Irini Doytchinova, Boryana Nikolova-Mladenova
article en
2 citations

Abstract

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.

MoleculesVol. 30(5)
Medical University of Sofia (BG)
Openalex Percentile: Top 17%
Synthesis and biological activity
1.87
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