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Abstract <p>A series of β-substituted N-heterocyclic phosphonium chlorides were prepared under mild stepwise reaction conditions without isolating of intermediate products. They exhibit high activity against two cancer cell lines (M-HeLa and HuTu 80), while having moderate cytotoxicity against normal cell line Wi38, as well as low hemolytic activity. The most active against human cervix epitheloid carcinoma (IC<sub>50</sub> = 7.1 µM) and human duodenal adenocarcinoma (IC<sub>50</sub> = 13.9 µM) was succinimide derivatives bearing alkyl or bicyclic substituents in heterocyclic core.</p>

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β-Substituted Triphenylphosphonium Chlorides with High Antitumor Activity Prepared by Step by Step Processes

  • 期刊论文

  • 发表日期：

    2026年5月2日

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  • Anton V. Il’in,
  • Mikhail A. Mamontov,
  • Vera N. Chupina,
  • Olga B. Babaeva,
  • Alexandra D. Voloshina,
  • Andrei V. Bogdanov

摘要

Abstract

A series of β-substituted N-heterocyclic phosphonium chlorides were prepared under mild stepwise reaction conditions without isolating of intermediate products. They exhibit high activity against two cancer cell lines (M-HeLa and HuTu 80), while having moderate cytotoxicity against normal cell line Wi38, as well as low hemolytic activity. The most active against human cervix epitheloid carcinoma (IC50 = 7.1 µM) and human duodenal adenocarcinoma (IC50 = 13.9 µM) was succinimide derivatives bearing alkyl or bicyclic substituents in heterocyclic core.