In Vitro Anticancer Activity
of <i>cis</i>-Diammineplatinum(II) Complexes with β-Diketonate
Leaving Group Ligands
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Abstract
Five cationic platinum(II) complexes of general formula,
[Pt(NH<sub>3</sub>)<sub>2</sub>(β-diketonate)]X are reported,
where X is a noncoordinating anion and β-diketonate = acetylacetonate
(acac), 1,1,1,-trifluoroacetylacetonate (tfac), benzoylacetonate (bzac),
4,4,4-trifluorobenzoylacetonate (tfbz), or dibenzoylmethide (dbm),
corresponding, respectively, to complexes <b>1</b>–<b>5</b>. The log <i>P</i> values and the stabilities of <b>1</b>–<b>5</b> in aqueous solution were evaluated.
The phenyl ring substituents of <b>3</b>–<b>5</b> increase the lipophilicity of the resulting complexes, whereas the
trifluoromethyl groups of <b>2</b> and <b>4</b> decrease
the stability of the complexes in aqueous solution. The uptake of <b>1</b>–<b>5</b> in HeLa cells increases as the lipophilicity
of the investigated complex increases. Cancer cell cytotoxicity studies
indicate that <b>1</b> and <b>3</b> are the least active
complexes whereas <b>2</b>, <b>4</b>, and <b>5</b> are comparable in activity to cisplatin
