Abstract

This paper presents the biological activity of copper(I) iodide complexes with 1,10-phenanthroline (phen) or 2,9-dimethyl-1,10-phenanthroline (dmp) and three tris (aminomethyl) phosphanes: P(CH 2N(CH 2CH 2) 2NCH 3) 3 ( 1), P(CH 2N(CH 2CH 2) 2O) 3 ( 2) and P (CH 2N(CH 3)CH 2CH 2OH) 3 ( 3). Crystallographic and DFT data indicate a significantly stronger binding ability of 3 in the complexes [CuI (phen) P (CH 2N (CH 3)CH 2CH 2OH) 3] ( 3P) and [CuI(dmp)P(CH 2N(CH 3)CH 2CH 2OH) 3] ( 3N) in comparison to the 1 or 2 ligands. Most probably, this is caused by the relatively small steric requirements of 3. The complexes with dmp exhibit a very high in vitro activity against the Staphylococcus aureus strain (MIC — minimal inhibitory concentration: 2.5–5 μg/mL) and Candida albicans diploid fungus (MIC: 1.25–2.5 μg/mL). All the tested complexes also show a strong in vitro antitumor activity against human ovarian carcinoma cell lines: MDAH 2774 (IC 50: 7–2 μM) and cisplatin-resistant SCOV 3 (IC 50: 3–2 μM). Interestingly, the complexes with dmp of higher biological activity more weakly interact with bovine serum albumin (BSA) and less efficiently cleave the pBluescriptSK+ plasmid.

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