Abstract
Cationic gold(I) complexes containing 1-[2-(acridin-9-ylamino)ethyl]-1,3-dimethylthiourea (1), [AuL(1)](n+) (where L is Cl(-), Br(-), SCN(-), PEt(3), PPh(3), or 1), derived from a class of analogous platinum(II) antitumor agents, have been synthesized. Unlike platinum, gold does not form permanent adducts with DNA, and its complexes are 2 orders of magnitude less cytotoxic in non-small-cell lung cancer cells than the most active platinum-based agent. Instead, several gold analogues show submicromolar and selective antimicrobial activity against Mycobacterium tuberculosis.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Acridines / chemical synthesis*
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Acridines / pharmacology
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Acridines / toxicity
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / toxicity
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Antitubercular Agents / chemical synthesis*
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Antitubercular Agents / pharmacology
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Antitubercular Agents / toxicity
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Biological Availability
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Chelating Agents / chemical synthesis
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Chlorocebus aethiops
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Coordination Complexes / chemical synthesis*
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Coordination Complexes / pharmacology
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Coordination Complexes / toxicity
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DNA Adducts / biosynthesis
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DNA, Bacterial / metabolism
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Drug Screening Assays, Antitumor
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Gold*
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Humans
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Ligands
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Mice
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Mycobacterium tuberculosis / drug effects*
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Organogold Compounds / chemical synthesis*
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Organogold Compounds / pharmacology
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Organogold Compounds / toxicity
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Platinum*
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Structure-Activity Relationship
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Thiourea / analogs & derivatives*
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Thiourea / chemical synthesis*
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Thiourea / pharmacology
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Thiourea / toxicity
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Urea / analogs & derivatives*
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Urea / chemical synthesis
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Urea / pharmacology
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Urea / toxicity
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Vero Cells
Substances
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1-(2-(acridin-9-ylamino)ethyl)-1,3-dimethylthiourea
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Acridines
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Antineoplastic Agents
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Antitubercular Agents
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Chelating Agents
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Coordination Complexes
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DNA Adducts
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DNA, Bacterial
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Ligands
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Organogold Compounds
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Platinum
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Gold
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Urea
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Thiourea