Domínguez-García, Moralba

Profile Picture

Filters

20121
Reset filters

Settings

Citations

Publication Search Results

Now showing 1 - 1 of 1
  • Thumbnail Image
    Publication
    Synthesis, characterization, cytotoxic activity and biological interactions of tungstenocene (lv) derivatives
    (2012) Domínguez-García, Moralba; Meléndez, Enrique; College of Arts and Sciences - Sciences; Cádiz, Mayra E.; Rivera, Nilka; Department of Chemistry; Orengo, Moises
    The design of medicinal compounds for cancer therapy is still a challenge. Organometallics offer a wide variety of promising anticancer drug candidates but this field is largely unexplored. This study has been focused on the development of modified tungstenocene complexes as new metal- based drugs, since little is known about them as anticancer agents. Four new complexes were synthesized in aqueous solution; [Cp2W(maltolato)]Cl, [Cp2W(ethylmaltolato)]Cl, [Cp2W(kojato)]Cl and Cp2W(malonate), their structures were elucidated and characterized by UV/Vis, IR, 1H-NMR spectroscopy, cyclic voltammetry and elemental analysis indicating that complexes contain bidentate ligands bound to W(IV), forming 5- and 6-membered chelating rings. Cytotoxic activity studies of the synthesized complexes were performed on HT-29 colon and MCF-7 breast cancer cells by MTT assay, where the new complexes showed higher cell inhibition (IC50 ~ 10-4 M) in comparison with tungstenocene dichloride (IC50 = 0.01 M) for HT- 29, whereas for MCF-7 all complexes showed inhibition concentrations of same order of magnitude (IC50 ~ 10-4 M).. The high solubility in water of the complexes should allow an easy transport into the cancer cell. Therefore, interaction studies were achieved with both human serum albumin and apo-transferrin proteins, to understand complexes delivery into the body and up to the cell. These studies were performed in Tris buffer solution at pH 7.4, using cyclic voltammetry and fluorescence techniques. The results suggest that there is an interaction, which is higher for new complexes than parent compound, based mainly in hydrophobic and electrostatic interactions. In conclusion, this study is the starting point for the development of new and promising tungstenocene (IV) derivatives as complexes with anticancer properties.