Abstract
A series of trans-platinum(IV) complexes with functionalized aromatic carboxylate ligands, cis,cis,trans-Pt(NH3)2Cl2(CO2C6H4R)2 (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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology
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Benzoates / chemistry*
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Cell Line, Tumor
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Chelating Agents / chemical synthesis
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Chelating Agents / pharmacology
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Crystallography, X-Ray
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Drug Resistance, Multiple
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Drug Resistance, Neoplasm
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Drug Screening Assays, Antitumor
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Humans
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Hydrogen Bonding
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Ligands
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Magnetic Resonance Spectroscopy
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Molecular Conformation
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Molecular Structure
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Organoplatinum Compounds / chemical synthesis*
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Organoplatinum Compounds / metabolism
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Organoplatinum Compounds / pharmacology
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Phthalic Acids / chemistry*
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Structure-Activity Relationship
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Antineoplastic Agents
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Benzoates
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Chelating Agents
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Ligands
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Organoplatinum Compounds
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Phthalic Acids