Actions of Metal Chelates of Substituted 1,10‐phenanthrolines on Viruses and Cells

Abstract

Summary. Metal chektes of 1, 10‐phenanthroline bases are lethal to cultured mammalian cells at concentrations as low as 10–7 molar. Chektes of Fe(II), Cu(II), Cd(II) and Ni(II) are more potent than those of Ru(II), which are highly stable and chemically inert. Activity is generally enhanced by increasing the number of methyl substituents in the phenanthroline ring or, in the case of Ru(II) chektes, by replacing one phenanthroline by an acetylacetonato ligand. There are striking differences between the chektes in the rapidity with which they kill cells Compounds containing Fe(II) or Ni(II), and those derived from unsubstituted 1,10‐phenanthroline, take days to initiate lethal changes at limit dilution. On the other hand, chektes containing Cd(II) or Cu(II) and hexamethylphenanthroline ligands, or Ru(II) together with the acetytacetonato ligand, initiate lethal cell damage that cannot be reversed following 2 hours’contact. A number of metal chektes actually prolong the survival of cells in culture at concentrations two to ten times lower than those damaging the cell. At cytocidal concentrations some depress the pH of the culture medium, whereas others increase it. By repeated passage of a mouse leukaemia cell line in the presence of acetykcetonato bis (3, 4, 7, 8‐tetramethyl‐1, 10‐phenanthroline) ruthenium (II) chloride, a stable mutant has been obtained which is resistant to ten times the dose of chekte lethal to the parental line. The correspondence between the cytocidal and virostatic titres of chektes in this and other cell lines suggests that these compounds inhibit virus multiplication by one of the mechanisms whereby they kill the cell.

In vivomeasurement of tissue oxygenation by time-resolved luminescence spectroscopy: advantageous properties of dichlorotris(1, 10-phenanthroline)-ruthenium(II) hydrate

“…26 Antitumoral and virostatic action of Ru-based polypyridyl complexes was observed both in vivo and in vitro 50 years ago. [27][28][29][30] Ru(Phen) is modestly cytotoxic (IC 50 ∼ 90 μmol∕l) and possesses relatively high clearance rate in vivo. [31][32][33] In general, in vivo toxicity strongly depends on the way of Ru(Phen) administration.…”

Reaction with DNA and pharmacologic activity of 1,10-phenanthroline and electron-rich 1,10-phenanthrocyanine complexes of d-elements

“…Among 2,2'-bipyridine and 1,10-phenanthroline derivatives, there are natural antibiotics, for example, caerulomycin А (4-methoxy-2,2'-bipyridyl-6-aldoxime) [63]. Antibacterial and antiviral effects of 1,10-phenanthroline, substituted 1,10-phenanthrolines, quaternary halides derived from N-alkyl-1,10-phenanthrolines, metal complexes of 1,10-phenanthrolines and its derivatives, as well as an antitumor effect of metal complexes of 1,10-phenanthrolines and their ability to kill dermatophytes have been reported [64][65][66][67][68][69][70][71].…”

Effect of the coordination centers and the solvents on the parameters of the 1H and 13C NMR spectra of biology active Zn+2 and Cd2+ acetate mononuclear complexes with chelating 1,10- phenanthroline

“…[Kr]4d 6 [Ru(phen) 3 ](ClO 4 ) 2 [21]. A systematic study of the antibacterial, antiviral, antimycotic and antitumor activity of 1,10-phenanthroline complexes was carried out in a subsequent series of studies [22][23][24][25][26][27]. They showed a relatively high biostatic effect of these compounds.…”