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Lipophilic gold(I) complexes with 1,3,4-oxadiazol-2-thione or 1,3-thiazolidine-2-thione moieties: synthesis and their cytotoxic and antimicrobial activities.
- Source :
-
Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine [Biometals] 2017 Dec; Vol. 30 (6), pp. 841-857. Date of Electronic Publication: 2017 Aug 24. - Publication Year :
- 2017
-
Abstract
- Novel lipophilic gold(I) complexes containing 1,3,4-oxadiazol-2-thione or 1,3-thiazolidine-2-thione derivatives were synthesized and characterized by IR, high resolution mass spectrometry, and <superscript>1</superscript> H, <superscript>13</superscript> C <superscript>31</superscript> P NMR. The cytotoxicity of the compounds was evaluated considering cisplatin and/or auranofin as reference in different tumor cell lines: colon cancer (CT26WT), metastatic skin melanoma (B16F10), breast adenocarcinoma (MCF-7), cervical carcinoma (HeLa), glioblastoma (M059 J). Normal human lung fibroblasts (GM07492-A) and kidney normal cell (BHK-21) were also evaluated. The gold(I) complexes were more active than their respective free ligands and cisplatin. Furthermore, antibacterial activity was evaluated against Gram-positive bacteria Staphylococcus aureus ATCC 25213, Staphylococcus epidermidis ATCC 12228 and Gram-negative bacteria Escherichia coli ATCC 11229 and Pseudomonas aeruginosa ATCC 27853 and expressed as the minimum inhibitory concentration (MIC). The complexes exhibited lower MIC values when compared to the ligands and chloramphenicol against Gram-positive bacteria and Gram-negative bacteria. Escherichia coli was sensitive one to the action of gold(I) complexes.
- Subjects :
- Animals
Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Line, Tumor
Chemistry Techniques, Synthetic
Cricetinae
Drug Evaluation, Preclinical
Escherichia coli drug effects
Humans
Magnetic Resonance Spectroscopy
Mice
Microbial Sensitivity Tests
Organogold Compounds chemical synthesis
Pseudomonas aeruginosa drug effects
Staphylococcus aureus drug effects
Structure-Activity Relationship
Thiones chemistry
Anti-Bacterial Agents pharmacology
Antineoplastic Agents pharmacology
Organogold Compounds chemistry
Organogold Compounds pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1572-8773
- Volume :
- 30
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine
- Publication Type :
- Academic Journal
- Accession number :
- 28840394
- Full Text :
- https://doi.org/10.1007/s10534-017-0046-6