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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Platinum(II)-Acyclovir Complexes: Synthesis, Antiviral and Antitumour Activity
M Coluccia1, A Boccarelli, C Cermelli
1Dipartimento di Scienze Biomediche e Oncologia Umana Piazza G. Cesare11 Bari 1-70124 Italy.
Metal-Based Drugs
|January 1, 1995
Summary
A novel platinum-acyclovir complex retains antiviral activity and shows anticancer potential, even against cisplatin-resistant leukemia. This dual-action compound exhibits distinct DNA interaction properties compared to cisplatin.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Molecular Biology
Background:
- A platinum(II) complex was synthesized using the antiviral drug acyclovir.
- The study aimed to compare its properties with acyclovir and cisplatin.
Purpose of the Study:
- To investigate the antiviral and anticancer properties of the platinum-acyclovir complex.
- To compare its efficacy and mechanism of action against acyclovir and cisplatin.
- To analyze its DNA interaction profile.
Main Methods:
- Synthesis of a platinum(II)-acyclovir complex.
- In vitro antiviral activity assays.
- In vivo anticancer efficacy studies in P388 leukemia models.
- DNA interaction studies (sequence specificity, interstrand cross-linking).
Main Results:
- The platinum-acyclovir complex maintained antiviral activity, though less potent than acyclovir on a molar basis.
- It showed anticancer efficacy comparable to cisplatin in vivo at equitoxic doses.
- The complex was effective against a cisplatin-resistant leukemia subline, suggesting a different mechanism of action.
- DNA interaction studies revealed distinct properties compared to cisplatin.
Conclusions:
- The platinum-acyclovir complex demonstrates potential as a dual-acting antiviral and anticancer agent.
- Its unique DNA interaction profile may overcome cisplatin resistance.
- Further investigation into this novel platinum complex is warranted.
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