Abstract
A series of polyfluorinated bipyridine cisplatins 2-6 were prepared, characterized, and evaluated for their in vitro cytotoxicities against a panel of human cancer cell lines, MCF7 (breast adenocarcinoma), MDA-MB-231 (breast adenocarcinoma) and A549 (lung adenocarcinoma). The results show that a correlation between the relative order of lipophilicity of complexes 2-4 and their cytotoxicity is established by following the trend: 4>2>3. Complex 4, which is the most active compound in the series, was found to be a more effective and selective anticancer agent than cisplatin. Complex 4 inhibited cancer cell proliferation by partial intercalation to DNA, which subsequently resulted in induction of S-G2/M arrest and apoptosis.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / analysis
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cell Cycle / drug effects*
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Cisplatin / analogs & derivatives
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Cisplatin / chemical synthesis*
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Cisplatin / chemistry
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Cisplatin / pharmacology
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Dose-Response Relationship, Drug
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Drug Design
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Drug Screening Assays, Antitumor
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Female
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Halogenation
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Humans
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Intercalating Agents / analysis
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Intercalating Agents / chemical synthesis*
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Intercalating Agents / chemistry
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Intercalating Agents / pharmacology
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M Phase Cell Cycle Checkpoints / drug effects
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Molecular Structure
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Pyridines / analysis
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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S Phase Cell Cycle Checkpoints / drug effects
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Software
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Tumor Cells, Cultured / cytology
Substances
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Antineoplastic Agents
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Intercalating Agents
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Pyridines
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Cisplatin