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Targeted Cancer Therapies

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Related Experiment Video

Updated: Jun 16, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

Towards Antitumor Active trans-Platinum Compounds.

Sheena M Aris¹, Nicholas P Farrell

¹Department of Chemistry, Virginia Commonwealth University 1001 W. Main St., Richmond VA 23284-2006.

European Journal of Inorganic Chemistry

|February 18, 2010

Summary

This summary is machine-generated.

New trans-platinum compounds show improved anticancer activity. These platinum-based drugs can form DNA-protein crosslinks, offering potential for targeted cancer therapies.

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Published on: February 12, 2017

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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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Published on: May 28, 2014

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Endobronchial Ultrasound-guided Intratumoral Injection of Cisplatin for the Treatment of Isolated Mediastinal Recurrence of Lung Cancer

Endobronchial Ultrasound-guided Intratumoral Injection of Cisplatin for the Treatment of Isolated Mediastinal Recurrence of Lung Cancer

Published on: February 12, 2017

Area of Science:

Medicinal Chemistry
Molecular Biology
Cancer Research

Background:

Cisplatin is a widely used platinum-based chemotherapy drug.
Transplatin, a related platinum compound, has historically shown limited efficacy.
Recent research explores modifications to transplatin to enhance its therapeutic properties.

Purpose of the Study:

To review the chemistry and biology of trans-platinum compounds with planar amines.
To assess the anticancer relevance of the trans-platinum geometry.
To explore the potential of trans-platinum chemotypes as selective DNA-protein crosslinking agents.

Main Methods:

Substitution of ammonia ligands in transplatin with various amines.
Analysis of cytotoxicity of resulting trans-platinum compounds.
Investigation of DNA adduct formation (intrastrand, interstrand) and DNA-protein crosslinking.
Study of protein interactions, specifically with zinc finger proteins.

Main Results:

Trans-platinum compounds with planar amines exhibit significantly improved cytotoxicity compared to transplatin, often matching cisplatin's efficacy.
The type of amine substituent influences the nature of bifunctional DNA adducts formed.
Monofunctional adducts are stable, leading to DNA-protein crosslink formation.
Trans-platinum compounds can interact with zinc finger proteins, potentially displacing zinc.

Conclusions:

The trans-platinum chemotype holds significant promise for developing novel anticancer agents.
These compounds demonstrate potential for selective DNA-protein crosslinking, a mechanism distinct from cisplatin.
Further research into trans-platinum interactions with DNA and proteins could lead to more targeted cancer therapies.