The salt metathesis reaction of sodium precursors, Na[H2B(mb)2] (Hmb = 2-mercapto-benzimidazole) and Na[H2B(mbt)2] (Hmbt = 2-mercapto-benzothiazole) of bipodal scorpionate ligands with Cu(OAc)2, CoCl2 and NiBr2 afforded six metal complexes, 1–6. The metal complexes were characterized using a combination of HR ESI-MS spectrometry, elemental analysis and IR spectroscopy. The cytotoxicity effect of these complexes was assessed on three human cancerous cell lines: MCF-7 (breast carcinoma), A549 (lung carcinoma) and SW1116 (colon adenocarcinoma) and compared with that for cis-platin. Our results indicated that all complexes had desirable antitumor activities (<100 µM). Copper complexes, 1 and 4, exhibited the highest anti-proliferative activity on all investigated cell lines, which are more effective than Ni and Co containing complexes and even cis-platin. The complex 1 also showed genotoxic effect and could effectively induce apoptosis in tumor cells. Molecular docking simulation studies on the synthesized complexes confirmed that 1 had the highest DNA-binding energy as their proposed targets, as well.

Cu(II), Ni(II) and Co(II) complexes with homoscorpionate Bis(2-Mercaptobenzimidazolyl) and Bis(2-Mercaptobenzothiazolyl)borate ligands: Synthesis and in vitro cytotoxicity studies

Piero Mastrorilli;Vito Gallo;
2020-01-01

Abstract

The salt metathesis reaction of sodium precursors, Na[H2B(mb)2] (Hmb = 2-mercapto-benzimidazole) and Na[H2B(mbt)2] (Hmbt = 2-mercapto-benzothiazole) of bipodal scorpionate ligands with Cu(OAc)2, CoCl2 and NiBr2 afforded six metal complexes, 1–6. The metal complexes were characterized using a combination of HR ESI-MS spectrometry, elemental analysis and IR spectroscopy. The cytotoxicity effect of these complexes was assessed on three human cancerous cell lines: MCF-7 (breast carcinoma), A549 (lung carcinoma) and SW1116 (colon adenocarcinoma) and compared with that for cis-platin. Our results indicated that all complexes had desirable antitumor activities (<100 µM). Copper complexes, 1 and 4, exhibited the highest anti-proliferative activity on all investigated cell lines, which are more effective than Ni and Co containing complexes and even cis-platin. The complex 1 also showed genotoxic effect and could effectively induce apoptosis in tumor cells. Molecular docking simulation studies on the synthesized complexes confirmed that 1 had the highest DNA-binding energy as their proposed targets, as well.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11589/204351
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • Scopus 2
  • ???jsp.display-item.citation.isi??? 2
social impact