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<p>The cytotoxic and antioxidant activity of 1,2,3,4-tetrahydropyridine-3,5-dicarboxylic acid (TDA) derivatives obtained by Mannich reactions of ethyl acetoacetate or ethyl 4,4-difluoroacetoacetate with formaldehyde and primary amines, including amino acid esters, was studied. The most active cytotoxic compound was fluorinated TDA with a tyrosine fragment, which showed a cytotoxic effect on HTC116 human colorectal carcinoma cells (IC<sub>50</sub> 70.25 μM). <i>N</i>-Propyl- and <i>N</i>-2-[(2-hydroxyethyl)amino]ethyl-TDA exhibited antioxidant properties in the FRAP model (EC<sub>50</sub> 12.03 and 11.83 μg/ml) that were comparable to those of ascorbic acid and Trolox.</p>

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In Vitro Cytotoxic and Antioxidant Activity of 1,2,3,4-Tetrahydropyridine-3,5-Dicarboxylic Acid Derivatives

  • 期刊论文

  • 发表日期：

    2026年1月1日

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  • N. N. Gibadullina,
  • A. R. Mukhamedyarova,
  • R. Yu. Khisamutdinova,
  • S. F. Gabdrakhmanova,
  • D. V. Ishmetova,
  • V. A. Vakhitov,
  • Yu. V. Vakhitova,
  • V. A. Dokichev

摘要

The cytotoxic and antioxidant activity of 1,2,3,4-tetrahydropyridine-3,5-dicarboxylic acid (TDA) derivatives obtained by Mannich reactions of ethyl acetoacetate or ethyl 4,4-difluoroacetoacetate with formaldehyde and primary amines, including amino acid esters, was studied. The most active cytotoxic compound was fluorinated TDA with a tyrosine fragment, which showed a cytotoxic effect on HTC116 human colorectal carcinoma cells (IC50 70.25 μM). N-Propyl- and N-2-[(2-hydroxyethyl)amino]ethyl-TDA exhibited antioxidant properties in the FRAP model (EC50 12.03 and 11.83 μg/ml) that were comparable to those of ascorbic acid and Trolox.