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

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.

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Publication Details

Journal
Russian Journal of General Chemistry
Published
2026-03-23
DOI
https://doi.org/10.1134/s1070363226600360
Primary Topic
Organophosphorus compounds synthesis
Type
article
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article

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

Anna P. Lyubina, Hoang Bao Tran Nguyen, A. M. Shakirov, Alexandra D. Voloshina et al.
Russian Journal of General Chemistry
Organophosphorus compounds synthesis
article

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

Anna P. Lyubina, Hoang Bao Tran Nguyen, A. M. Shakirov, Alexandra D. Voloshina, A. R. Burilov, Elmira M. Gibadullina, Timur R. Shaekhov, Anna G. Strelnik
article en

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.

Russian Journal of General ChemistryVol. 96(4)
A.E. Arbuzov Institute of Organic and Physical Chemistry (RU), Kazan State Technological University (RU)
Openalex Percentile: Top 11%
Organophosphorus compounds synthesis
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