title: Biological activity and structure dependent properties of cuprous iodide complexes with phenanthrolines and water soluble tris (aminomethyl) phosphanes.
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(CH2N(CH2CH2)2NCH3)3 (1), P(CH2N(CH2CH2)2O)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 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 (IC50: 7-2 μM) and cisplatin-resistant SCOV3 (IC50: 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.
authors: Faculty of Chemistry, Department of Genetics, University of Wroclaw, F. Joliot-Curie 14, 50-383 Wrocław, Poland. starosta@wchuwr.pl
authors: Radosław
authors: R
authors: Starosta
authors: Kamila
authors: K
authors: Stokowa
authors: Magdalena
authors: M
authors: Florek
authors: Jarosław
authors: J
authors: Król
authors: Agnieszka
authors: A
authors: Chwiłkowska
authors: Julita
authors: J
authors: Kulbacka
authors: Jolanta
authors: J
authors: Saczko
authors: Jacek
authors: J
authors: Skała
authors: Małgorzata
authors: M
authors: Jeżowska-Bojczuk
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D045744:Cell Line, Tumor; D003300:Copper / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D007454:Iodides / Q000737:chemistry* / Q000494:pharmacology; D008024:Ligands; D010618:Phenanthrolines / Q000737:chemistry / Q000494:pharmacology; D010720:Phosphines / Q000737:chemistry* / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D014867:Water
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D007454:Iodides; D008024:Ligands; D010618:Phenanthrolines; D010720:Phosphines; D014867:Water; D003300:Copper; C073870:cuprous iodide; C044646:phosphine