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Abstract <p>A series of novel betulin-28-thiazole ester derivatives were designed, synthesized, and subsequently evaluated for their anticancer activity. Among these compounds, 3β-hydroxylup-20(29)-en-28-yl 3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide demonstrated the most potent anticancer activity against A549 cells, with an IC<sub>50</sub> value of 2.24 µM, being 11.23-fold more potent than betulin. Meanwhile, 3β-hydroxylup-20(29)-en-28-yl 3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide displayed exceptional water solubility, being 20.15-fold higher than that of betulin. In summary, these data identified 3β-hydroxylup-20(29)-en-28-yl-3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide as a promising lead compound that warrants further investigation of its anticancer properties.</p>

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Design and Synthesis of Novel Betulin Derivatives Containing Thiazole Moiety as Anticancer Agents

  • 期刊论文

  • 发表日期：

    2025年3月27日

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  • Y. B. Zhang,
  • S. W. Pan,
  • M. Zhang,
  • X. S. Guo,
  • J. F. Wang,
  • M. Bu

摘要

Abstract

A series of novel betulin-28-thiazole ester derivatives were designed, synthesized, and subsequently evaluated for their anticancer activity. Among these compounds, 3β-hydroxylup-20(29)-en-28-yl 3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide demonstrated the most potent anticancer activity against A549 cells, with an IC50 value of 2.24 µM, being 11.23-fold more potent than betulin. Meanwhile, 3β-hydroxylup-20(29)-en-28-yl 3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide displayed exceptional water solubility, being 20.15-fold higher than that of betulin. In summary, these data identified 3β-hydroxylup-20(29)-en-28-yl-3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide as a promising lead compound that warrants further investigation of its anticancer properties.