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Palladium and platinum famotidine complexes.

G B Onoa¹, V Moreno

¹Departament de Química Inorgànica, Universitat de Barcelona, Spain.

Journal of Inorganic Biochemistry

|March 5, 1999

Summary

Famotidine metal complexes show potential anticancer activity. Palladium and platinum derivatives were synthesized, with the platinum complex forming a dimer that alters DNA conformation but exhibits limited cytotoxicity against cancer cells.

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Area of Science:

Coordination chemistry
Medicinal inorganic chemistry
Cancer research

Background:

Famotidine, an ulceration inhibitor, demonstrates strong coordination abilities with transition metal ions.
Specific binding sites on famotidine include guanidine, amine, thiazole nitrogen, and thioether sulfur.

Purpose of the Study:

To synthesize and structurally characterize palladium (Pd(II)) and platinum (Pt(II)) derivatives of famotidine.
To investigate the potential antitumor activity of these famotidine-metal complexes, particularly the platinum dimer.

Main Methods:

Synthesis of Pd(II) and Pt(II) famotidine complexes.
Structural analysis of the complexes.
Assays examining DNA conformation changes using circular dichroism (CD), interstrand crosslinking, and electrophoretic mobility.
Cytotoxicity studies using U937 human leukemia and HeLa human womb carcinoma cell lines.

Main Results:

Palladium complex identified as a monomer; platinum complex forms a dimer.
Both complexes induced changes in DNA conformation.
The platinum complex demonstrated only a small antiproliferative effect on tested cancer cell lines.

Conclusions:

Famotidine effectively coordinates with transition metals, forming distinct monomeric (Pd) and dimeric (Pt) complexes.
While the platinum complex interacts with DNA, its observed cytotoxicity is limited, suggesting further research is needed for therapeutic applications.

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