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Updated: Aug 2, 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
Beyond mere DNA damage: Recent progress in platinum(IV) anticancer complexes containing multi-functional axial
1Department of Chemistry, City University of Hong Kong, Hong Kong SAR, PR China; City University of Hong Kong Shenzhen Research Institute, Shenzhen, 518057, PR China.
Platinum(IV) prodrugs offer enhanced anticancer performance by overcoming limitations of traditional platinum(II) drugs. Axial ligand modification enables multi-functional platinum(IV) complexes for next-generation cancer therapies.
Area of Science:
- Medicinal Chemistry
- Nanotechnology
- Drug Discovery
Background:
- Platinum-based anticancer drugs are clinically significant.
- Platinum(IV) prodrugs show promise as successors to platinum(II) drugs.
- Modification of axial ligands in platinum(IV) complexes offers unique therapeutic advantages.
Purpose of the Study:
- To review recent advancements in platinum(IV) anticancer complexes.
- To highlight the axial functionalization of platinum(IV) complexes.
- To guide the design of next-generation multi-functional platinum(IV) anticancer agents.
Main Methods:
- Summarizing recent developments in platinum(IV) coordination chemistry.
- Focusing on axial ligand functionalization strategies.
- Reviewing applications with anticancer, immunotherapeutic, photosensitive, peptide, and theranostic agents.
Main Results:
- Judicious axial ligand modification of platinum(IV) complexes yields unique properties.
- Platinum(IV) complexes can be functionalized with diverse agents (anticancer, immunotherapy, photosensitizers, peptides, theranostics).
- These modifications enable overcoming limitations of conventional platinum(II) drugs.
Conclusions:
- Platinum(IV) complexes represent a versatile platform for developing advanced anticancer drugs.
- Axial functionalization is key to creating multi-functional platinum(IV) agents.
- This review provides insights for designing next-generation platinum(IV)-based cancer therapeutics.
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