Biological activity and structure dependent properties of cuprous iodide complexes with phenanthrolines and water soluble tris (aminomethyl) phosphanes

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(CH2N(CH2CH2)(2) NCH3)(3) (1). P(CH2N(CH2CH2)(2)O)(3) (2) and P (CH2N(CH3)CH2CH2OH)(3) (3). Crystallographic and DFT data indicate a significantly stronger binding ability of 3 in the complexes [CuI (phen) P (CH2N (CH3)CH2CH2OH)(3)] (3P) and [CuI(dmp)P(CH2N(CH3)CH2CH2OH)(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 mu g/mL) and Candida albicans diploid fungus (MIC: 1.25-2.5 mu g/mL). All the tested complexes also show a strong in vitro antitumor activity against human ovarian carcinoma cell lines: MDAH 2774 (IC50: 7-2 mu m) and cisplatin-resistant SCOV 3 (IC50: 3-2 mu M). Interestingly, the complexes with dmp of higher biological activity more weakly interact with bovine serum albumin (BSA) and less efficiently cleave the pBluescriptSK+ plasmid. (C) 2011 Elsevier Inc. All rights reserved.