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Abstract <p>Despite several approved chemotherapeutic agents, the mortality rate from breast cancer remains high. Two tetraorganylammonium and two organyltriphenylphosphonium platinum (IV) compounds were synthesized in relatively high yield. The crystal structures were resolved, and the complexes were characterized using infrared and NMR spectroscopy. All four complexes were tested for their ability to inhibit cancer cell proliferation using the MCF–7 breast cancer cell line. Quantum chemistry calculations yielded geometries in a water solution. Of the four compounds, <b>AV1</b> showed the highest inhibitory potential with an experimentally determined IC<InlineEquation ID="IEq1"> <EquationSource Format="TEX">\(_{50}\)</EquationSource> </InlineEquation> value of 10.3 <InlineEquation ID="IEq2"> <EquationSource Format="TEX">\(\mu \)</EquationSource> </InlineEquation>g/mL, which is lower compared to the standard drug dasatinib (20.8 <InlineEquation ID="IEq3"> <EquationSource Format="TEX">\(\mu \)</EquationSource> </InlineEquation>g/mL) for breast cancer cell lines. Available QSAR models identified topoisomerase I as a potential target for <b>AV1</b>. <i>In vivo</i> experiments confirmed that mitochondrial parameters improved in rats with DMBA-induced breast cancer treated with <b>AV1</b> compared with the control group. In addition, <b>AV1</b> suppresses cytokine levels and exhibits antioxidant activity. The synthesis and characterization of new platinum(IV) complexes, featuring distorted tetrahedral cations and octahedral anions, are presented. <b>AV1</b> exhibited superior anti-cancer activity against breast cancer cells compared to <b>AV2</b>, <b>AV3</b>, and <b>AV4</b>, alongside demonstrating chemoprotective effects in DMBA-induced breast cancer models. Further investigation is warranted to elucidate the underlying mechanisms.</p> Graphic Abstract <p></p>

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The Synthesis, in Silico Characterization and in Vitro and in Vivo Evaluation of Platinum (IV) Complexes as Potential Breast-Cancer Treatments

  • 期刊论文

  • 发表日期：

    2026年3月24日

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  • Jurica Novak,
  • Alena R. Zykova,
  • Vikas Kumar,
  • Vladimir V. Sharutin,
  • Olga K. Sharutina,
  • Ashok Kumar,
  • Khalid M. AlGhamdi,
  • Kristina Kraljić,
  • Amita Verma

摘要

Abstract

Despite several approved chemotherapeutic agents, the mortality rate from breast cancer remains high. Two tetraorganylammonium and two organyltriphenylphosphonium platinum (IV) compounds were synthesized in relatively high yield. The crystal structures were resolved, and the complexes were characterized using infrared and NMR spectroscopy. All four complexes were tested for their ability to inhibit cancer cell proliferation using the MCF–7 breast cancer cell line. Quantum chemistry calculations yielded geometries in a water solution. Of the four compounds, AV1 showed the highest inhibitory potential with an experimentally determined IC \(_{50}\) value of 10.3 \(\mu \) g/mL, which is lower compared to the standard drug dasatinib (20.8 \(\mu \) g/mL) for breast cancer cell lines. Available QSAR models identified topoisomerase I as a potential target for AV1. In vivo experiments confirmed that mitochondrial parameters improved in rats with DMBA-induced breast cancer treated with AV1 compared with the control group. In addition, AV1 suppresses cytokine levels and exhibits antioxidant activity. The synthesis and characterization of new platinum(IV) complexes, featuring distorted tetrahedral cations and octahedral anions, are presented. AV1 exhibited superior anti-cancer activity against breast cancer cells compared to AV2, AV3, and AV4, alongside demonstrating chemoprotective effects in DMBA-induced breast cancer models. Further investigation is warranted to elucidate the underlying mechanisms.

Graphic Abstract