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Abstract <p>A method for the synthesis of 3,4-diaryl-5-morpholinoisoxazoles was developed, featuring the optimization of reaction conditions to introduce a morpholine moiety at the 5-position of 5-chloroisoxazoles. The representative compound <b>9</b> was prepared and evaluated <i>in vitro</i>, demonstrating moderate water solubility along with cytotoxic activity against selected cell lines. This modification strategy provides a viable approach for further structural diversification of combretastatin A4 analogues within the isoxazole series, enabling the expansion of a library of heterocyclic derivatives with improved physicochemical properties.</p>

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Synthesis and Cytotoxic Properties of 3,4-Diaryl-5-morpholinoisoxazole as an Analogue of Combretastatin A4

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年4月28日

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  • Georgy L. Karetnikov,
  • Dmitry A. Guk,
  • Anastasiia A. Filatova,
  • Margarita A. Vorobeva,
  • Dmitry A. Skvortsov,
  • Oksana B. Bondarenko

摘要

Abstract

A method for the synthesis of 3,4-diaryl-5-morpholinoisoxazoles was developed, featuring the optimization of reaction conditions to introduce a morpholine moiety at the 5-position of 5-chloroisoxazoles. The representative compound 9 was prepared and evaluated in vitro, demonstrating moderate water solubility along with cytotoxic activity against selected cell lines. This modification strategy provides a viable approach for further structural diversification of combretastatin A4 analogues within the isoxazole series, enabling the expansion of a library of heterocyclic derivatives with improved physicochemical properties.