Newly synthesized palladium (II) complexes with aminothiazole derivatives: in vitro study of antimicrobial and antitumor activity in the human prostate cancer cell line
This article was originally published here
Dalton Trans. December 24, 2021. doi: 10.1039 / d1dt03364f. Online ahead of print.
Five new complexes of the palladium (II) ion (C1-C5) of general formula [(PdL2)]Cl2 with some 2-aminothiazoles (L1-L5), where L1 = 2-amino-4- (3,4-difluorophenyl) thiazole, L2 = 2-amino-5-methyl-4-phenylthiazole, L3 = 2-amino-4 -phenylthiazole, L4 = 2-amino-4- (4-chlorophenyl) thiazole, and L5 = 2-amino-4- (2,4-difluorophenyl) thiazole, were synthesized and characterized by elemental and infrared microanalysis, 1H NMR and 13C. le NMR spectroscopy in vitro the antimicrobial activity of the five ligands and the corresponding Pd (II) complexes is studied. The tests are performed by the microdilution method and the minimum inhibitory concentration (MIC) and minimum microbicidal concentration (MWC) have been determined. Tests are being carried out against 11 microorganisms (nine strains of pathogenic bacteria and two species of yeast). The ligands and palladium (II) complexes tested exhibit selective, high and moderate activity. There is a difference in antimicrobial activity between the ligands and the corresponding palladium (II) complexes. The complexes have significant anti-staphylococcal activity and activity on Pseudomonas aeruginosa which is better than the positive control. The interactions of newly synthesized palladium (II) complexes with calf thymus DNA (DNA-CT) were investigated using UV-Vis absorption and fluorescence spectroscopy. Analysis of UV absorption and fluorescence spectra indicate the formation of a complex between the palladium (II) complexes and DNA. The high values of the intrinsic binding constants, Kb, of the order of 104 M-1 and Stern-Volmer extinction constants, KSV, of the order of 105 M-1 indicated very good binding of all complexes to DNA-CT. In addition, the novel Pd (II) complexes show high cytotoxic activity towards the human prostate cancer cell line and insignificant activity towards non-cancerous human fibroblasts. Future research could further explore the biological activity of the Pd (II) complexes presented in this article and investigate the possibility of their implementation in clinical practice.
PMID: 34951416 | DOI: 10.1039 / d1dt03364f