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Abstract <p>The synthesis of new acylhydrazones based on derivatives of phosphorylacetic acids and 2,3-dihydroxybenzaldehyde was performed. Their antibacterial and cytotoxic activity was studied. Many of the prepared compounds surpass sorafenib in activity against M-HeLa cells. 2-Chloroethyl (<i>E</i>)-(4-diethylaminophenyl)-{2-[2-(2,3-dihydroxy-4,6-dicyclohexylbenzylidene)hydrazinyl]-2-oxoethyl}phosphinate showed selectivity towards tumor cells. The relationship between lipophilicity and antitumor effect was revealed. The results confirm the promise of the obtained acylhydrazones as potential selective antitumor agents.</p>

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Synthesis and Biological Activity of Sterically Hindered Phenolic Derivatives of Phosphorylacetic Acid Hydrazides

  • 期刊论文

  • 发表日期：

    2026年5月25日

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  • Roza G. Tagasheva,
  • Sergey V. Bukharov,
  • Dinara M. Zamaletdinova,
  • Alexandra D. Voloshina,
  • Andrei V. Bogdanov,
  • Maksim V. Arsenyev,
  • Elena L. Gavrilova

摘要

Abstract

The synthesis of new acylhydrazones based on derivatives of phosphorylacetic acids and 2,3-dihydroxybenzaldehyde was performed. Their antibacterial and cytotoxic activity was studied. Many of the prepared compounds surpass sorafenib in activity against M-HeLa cells. 2-Chloroethyl (E)-(4-diethylaminophenyl)-{2-[2-(2,3-dihydroxy-4,6-dicyclohexylbenzylidene)hydrazinyl]-2-oxoethyl}phosphinate showed selectivity towards tumor cells. The relationship between lipophilicity and antitumor effect was revealed. The results confirm the promise of the obtained acylhydrazones as potential selective antitumor agents.