Investigation of the pharmacological profiles of dinuclear metal complexes as novel, potent and selective cytotoxic agents against ras -transformed cells

•New Au(III) and Ru(II) complexes were prepared.•The compounds were characterized by 1H NMR, IR, MS, and elemental analysis.•Complexes are very stable and they can easily soluble in DMSO at small volumes.•It is cytotoxic and apoptotic activities were determined.•Au(III) complex has selective toxicit...

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Veröffentlicht in:Environmental toxicology and pharmacology 2014-05, Vol.37 (3), p.897-906
Hauptverfasser: Bostancıoğlu, R. Beklem, Koparal, A. Tansu, Benkli, Kadriye
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Sprache:eng
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Zusammenfassung:•New Au(III) and Ru(II) complexes were prepared.•The compounds were characterized by 1H NMR, IR, MS, and elemental analysis.•Complexes are very stable and they can easily soluble in DMSO at small volumes.•It is cytotoxic and apoptotic activities were determined.•Au(III) complex has selective toxicity on cancer cells even in low concentrations. Around the world scientists try to design successful cures against still incurable diseases, especially cancers. New targets for prevention and new agents for therapy need to be identified. We synthesized novel metal complexes [Au(L1)(L2)Pt]Cl2 and [Ru(L1)2(L2)Pt]Cl2 for determining their cytotoxic and apoptotic effects. The complexes are synthesized by using 1,8-diaminonaphthalene (L1), and bis-1,4-di[([1,10]phenanthroline-5-il)aminomethyl]cyclohexane (L2) as ligands. This is the first study to examine these metals and these molecules in cancer treatment. We elucidated the effects of test compounds with embryonic rat fibroblast-like cells (F2408) and H-ras oncogene activated embryonic rat fibroblast-like cancer cells (5RP7). Results showed that our complexes are more effective than cisplatin to kill ras-transformed cells. Although the [Au(L1)(L2)Pt]Cl2 compound showed a cytotoxic potency higher than [Ru(L1)2(L2)Pt]Cl2 against cancer cells, it proved to be almost five times less effective in decreasing cell viability over healthy cells. Au(III) compound selectively targets the cancer cells but not the healthy cells.
ISSN:1382-6689
1872-7077
DOI:10.1016/j.etap.2014.03.003