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EPFL > infoscience > Synthesis and characterization of platinum(IV) anticancer drugs with functionalized aromatic carboxylate ligands: Influence of the ligands on drug efficacies and uptake.
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Ang, WH ; Pilet, S ; Scopelliti, R ; Bussy, F ; Juillerat-Jeanneret, L ; Dyson, PJ In: JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, num. 25, 2005, p. 8060-8069 Date: 2005 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. Reference: LCOM-ARTICLE-2006-012 |
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Record created on 2006-02-13, modified on 2009-10-27 |
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