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<p>A novel combretastatin A-4 (CA-4) analog [4-(4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)isoxazole, A-123124] has been synthesized. Its physical and chemical characteristics, <i>in vitro</i> cytotoxic activity using human and murine tumor cells, tolerability, and antitumor activity on mice with transplanted human and murine tumors have been studied. The <i>in vitro</i> activity of A-123124 was 10 – 100 times higher than those of the reference compounds CA-4P (di-Na salt) and paclitaxel in the medicine Paclitaxel Ebewe<sup>®</sup>. Human (HCT-116) and murine colon tumors (C-26) were most sensitive to therapy with the CA-4 analog <i>in vivo</i>. Tumor growth inhibition and the increase in the lifespan of treated animals differed statistically significantly from the control data and were almost biologically significant. Combination of the treatment with radiation significantly prolonged the animal lifespans. It was concluded that the synthesized compound was quite promising for further research on the development of a dosage form with improved bioavailability.</p>

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Diaryl Isoxazole Analog of Combretastatin A4 (A Promising Substance for an Antitumor Drug

  • 期刊论文

  • 发表日期：

    2025年1月1日

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  • E. R. Nemtsova,
  • N. B. Morozova,
  • A. D. Plyutinskaya,
  • A. N. Noev,
  • A. A. Pankratov,
  • D. V. Demchuk,
  • S. S. Krylov,
  • V. V. Semenov,
  • P. V. Shegay,
  • A. D. Kaprin

摘要

A novel combretastatin A-4 (CA-4) analog [4-(4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)isoxazole, A-123124] has been synthesized. Its physical and chemical characteristics, in vitro cytotoxic activity using human and murine tumor cells, tolerability, and antitumor activity on mice with transplanted human and murine tumors have been studied. The in vitro activity of A-123124 was 10 – 100 times higher than those of the reference compounds CA-4P (di-Na salt) and paclitaxel in the medicine Paclitaxel Ebewe®. Human (HCT-116) and murine colon tumors (C-26) were most sensitive to therapy with the CA-4 analog in vivo. Tumor growth inhibition and the increase in the lifespan of treated animals differed statistically significantly from the control data and were almost biologically significant. Combination of the treatment with radiation significantly prolonged the animal lifespans. It was concluded that the synthesized compound was quite promising for further research on the development of a dosage form with improved bioavailability.