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Abstract <p>A method was developed for the preparation of polychloroalkyl derivatives of diarylmethylphosphonates containing a sterically hindered phenol using 3-chloro-2,2-bis(chloromethyl)propanoyl chloride. Primary biological screening revealed low background cytotoxicity for most compounds, consistent with the profile of redox-activated prodrugs, while two derivatives exhibited moderate activity. The developed approach provides a basis for the targeted search for new selective anticancer agents based on modified sterically hindered phenols.</p>

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Diarylmethylphosphonates Containing a Sterically Hindered Phenol and Terminal Amino Groups in the Synthesis of Polychloroalkyl Diamides

  • 期刊论文

  • 发表日期：

    2026年3月23日

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  • Hoang Bao Tran Nguyen,
  • Adel M. Shakirov,
  • Timur R. Shaekhov,
  • Anna G. Strelnik,
  • Anna P. Lyubina,
  • Elmira M. Gibadullina,
  • Aleksandra D. Voloshina,
  • Aleksandr R. Burilov

摘要

Abstract

A method was developed for the preparation of polychloroalkyl derivatives of diarylmethylphosphonates containing a sterically hindered phenol using 3-chloro-2,2-bis(chloromethyl)propanoyl chloride. Primary biological screening revealed low background cytotoxicity for most compounds, consistent with the profile of redox-activated prodrugs, while two derivatives exhibited moderate activity. The developed approach provides a basis for the targeted search for new selective anticancer agents based on modified sterically hindered phenols.