Abstract
Four highly charged, water soluble platinum-acridine bisintercalating agents have been synthesized. Depending on the cis/trans isomerism of the metal and the nature of the acridine side chains, bisintercalation induces/stabilizes the classical Watson-Crick B-form or a non-B-form. Circular dichroism spectra and chemical footprinting experiments suggest that 4, the most active derivative in HL-60 cells, produces a structurally severely perturbed DNA with features of a Hoogsteen base-paired biopolymer.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Acridines / chemistry*
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Acridines / pharmacology
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Chelating Agents / chemistry*
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Circular Dichroism
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DNA / chemistry*
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HL-60 Cells
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Humans
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Intercalating Agents / chemistry*
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Intercalating Agents / pharmacology
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Nucleic Acid Conformation
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Platinum*
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Polydeoxyribonucleotides / chemistry
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Solubility
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Stereoisomerism
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Water
Substances
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Acridines
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Antineoplastic Agents
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Chelating Agents
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Intercalating Agents
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Polydeoxyribonucleotides
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Water
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poly(dC-dG)
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Platinum
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DNA