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Updated: Oct 25, 2025
Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Advancements in the Use of Platinum Complexes as Anticancer Agents
Rajiv Sharma1, Vikram Jeet Singh2, Pooja A Chawla2
1University Institute of Pharma Sciences, Chandigarh University, Mohali, India.
Background:
The platinum (II) complexes as anticancer agents have been well explored for the development of novel analogs. Yet, none of them achieved clinical importance in oncology. At present, anticancer compounds containing platinum (II) complexes have been employed in the treatment of colorectal, lung, and genitourinary tumors. Among the platinum-based anticancer drugs, Cisplatin (cis-diamine dichloroplatinum (II), cis-[Pt(NH3)2Cl2]) is one of the most potent components of cancer chemotherapy. The nephrotoxicity, neurotoxicity and ototoxicity, and platinum compounds associated resistant cancer are some major disadvantages.
Objective:
With the rapidly growing interest in platinum (II) complexes in tumor chemotherapy, researchers have synthesized many new platinum analogs as anticancer agents that show better cytotoxicity, and less off-target effects with less cellular resistance. This follows the introduction of oxaliplatin, water-soluble carboplatin, multinuclear platinum and newly synthesized complexes, etc. Methods: This review emphasizes recent advancements in drug design and development, the mechanism of platinum (II) complexes, their stereochemistry, current updates, and biomedical applications of platinum-based anticancer agents.
Conclusion:
In the last few decades, the popularity of platinum complexes as potent anti-cancer agents has risen as scientists have synthesized many new platinum complexes that exhibit better cytotoxicity coupled with less off-target effects.
Insights
Platinum (II) complexes are vital anticancer agents, but limitations like toxicity and resistance persist. Ongoing research focuses on developing novel platinum analogs with improved efficacy and reduced side effects for cancer chemotherapy.
Area of Science:
- Medicinal Chemistry
- Oncology
- Drug Discovery
Background:
- Platinum (II) complexes are established anticancer agents used for colorectal, lung, and genitourinary tumors.
- Cisplatin (cis-diamine dichloroplatinum (II), cis-[Pt(NH3)2Cl2]) is a potent chemotherapy drug but has significant drawbacks including nephrotoxicity, neurotoxicity, ototoxicity, and resistance.
- Despite their efficacy, many platinum (II) complexes have not achieved widespread clinical importance due to these limitations.
Purpose of the Study:
- To review recent advancements in the design and development of platinum (II) complexes as anticancer agents.
- To explore the mechanisms of action, stereochemistry, and biomedical applications of these compounds.
- To highlight strategies for overcoming resistance and reducing off-target effects.
Main Methods:
- This review synthesizes information from recent scientific literature on platinum (II) complexes.
- It focuses on advancements in drug design, understanding mechanisms, and exploring new analogs.
- The review covers stereochemistry, current updates, and biomedical applications.
Main Results:
- Numerous novel platinum analogs have been synthesized, demonstrating enhanced cytotoxicity and reduced off-target effects compared to older agents.
- Developments include oxaliplatin, water-soluble carboplatin, and multinuclear platinum complexes.
- These new agents show promise in overcoming cellular resistance and improving therapeutic outcomes.
Conclusions:
- The field of platinum (II) complexes for cancer chemotherapy continues to evolve rapidly.
- Newer platinum analogs offer improved efficacy and safety profiles.
- Continued research in drug design and understanding mechanisms is crucial for developing next-generation anticancer therapies.
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