Synthesis and characterization of platinum(IV) anticancer drugs with functionalized aromatic carboxylate ligands: Influence of the ligands on drug efficacies and uptake

A series of trans-platinum(IV) complexes with functionalized aromatic carboxylate ligands, cis,cis,trans-Pt(NH<sub>3</sub>)<sub>2</sub>Cl<sub>2</sub>(CO<sub>2</sub>C<sub>6</sub>H<sub>4</sub>R)<sub>2</sub> (R = H (3), p-vinyl (4), p-methoxy (5), p-iodo (6), p-cyano (7), or o-carboxyl (8)) was synthesized and characterized by spectroscopic methods. Crystal structures of 3, 4, 7, and 8 were obtained, which revealed that their structural conformations were influenced by intramolecular H-bonding interactions. The complexes were evaluated for cellular uptake and inhibition of cell proliferation against a panel of lung, colon, and breast carcinoma cell lines. The functionalization of the aromatic carboxylate ligand was found to have a profound influence on the uptake, and hence, efficacy, of this class of complex.


Published in:
JOURNAL OF MEDICINAL CHEMISTRY, 48, 25, 8060-8069
Year:
2005
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 Record created 2006-02-13, last modified 2018-03-17


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