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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
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Multi-specific niflumic acid platinum(IV) complexes displaying potent antitumor activities by improving immunity and

Linming Li1, Ming Zhang1, Dianlong Jia2

  • 1Institute of Biopharmaceutical Research, Liaocheng University, Liaocheng 252059, P.R. China. lywqp@126.com.

Dalton Transactions (Cambridge, England : 2003)
|December 6, 2022
PubMed

Insights

New platinum(IV) complexes combining niflumic acid show potent anti-tumor and anti-metastasis effects. These novel agents damage tumor DNA, activate immune responses, and suppress blood vessel growth, offering a promising new cancer therapy.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Immunotherapy

Background:

  • Developing novel chemotherapeutics with anti-metastasis properties is crucial for improving cancer treatment outcomes.
  • Platinum-based drugs are widely used, but resistance and toxicity remain challenges.
  • Multi-specific agents targeting various cancer hallmarks offer a promising therapeutic strategy.

Purpose of the Study:

  • To design, synthesize, and evaluate novel multi-specific niflumic acid (NFA) platinum(IV) complexes as antitumor agents.
  • To investigate the anti-metastasis properties and underlying mechanisms of these novel complexes.
  • To assess the efficacy and toxicity profile compared to existing platinum drugs.

Main Methods:

  • Synthesis and characterization of multi-specific NFA platinum(IV) complexes.
  • In vitro and in vivo evaluation of antitumor activities.
  • Analysis of DNA damage, apoptosis, immune cell infiltration, and angiogenesis suppression.

Main Results:

  • A dual NFA platinum(IV) complex with a cisplatin core demonstrated significant in vitro and in vivo antitumor activity with reduced toxicity.
  • The complex induced DNA damage (elevated γ-H2AX), promoted apoptosis via mitochondrial pathways and autophagy.
  • Tumor immune response was enhanced (increased CD3+, CD4+, CD8+ T cells), and angiogenesis was suppressed (reduced CD34+ microvessels) by inhibiting the ERK/HIF-1α/VEGFA pathway.

Conclusions:

  • Multi-specific NFA platinum(IV) complexes exhibit potent anti-proliferative and anti-metastatic properties.
  • These complexes offer a multi-targeted approach with potential for improved cancer therapy.
  • Further development of these novel platinum(IV) complexes as anti-cancer drugs is warranted.

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