Lamboy Vega, José L.

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    Synthesis, chemical and biochemical characterization of Tiᴵⱽ and Vᴵⱽ complexes with anti-tumor activity
    (2010) Lamboy Vega, José L.; Meléndez, Enrique; College of Arts and Sciences - Sciences; Cortés, José; Román, Felix; Department of Chemistry; Calcagno, Barbara
    At the present time in which the metallocene dihalides have shown to possess antitumoral activity, scientists of all around the world have been working with the synthesis and structural modifications to improve their performance. This work was aimed to the synthesis and chemical/biochemical characterization of the titanium and vanadium complexes. Two complexes were synthetisized Ti(maltolato)₂(OH)₂ and V(maltolato)₂Cl₂, using as starting material titanocene and vanadocene dichlorides respectively. The characterization of both complexes was achieved using techniques as Infrared spectroscopy (IR), Nuclear Magnetic Resonance (NMR), Mass spectroscopy (MS), and Cyclic Voltammetry (CV) among others. Interaction studies between these complexes with apo-transferrin, using UV-VIS, showed that vanadium complex has the capacity to bind the biomolecule by donation of V(IV) to apo-transferrin bindin pocket. The titanium-maltol complex showed to be a robust one because does not donate the metal to apo-transferrin. Neither the titanium or vanadium complexes interact with the DNA molecule or oligonucleotide. Cytotoxic studies using HT-29 cancer cells showed that Ti(maltolato)2(OH)2 was the most active complex in comparison with other eight complexes including titanocene [¹]. Ti(maltolato)₂(OH)₂ shows hydrolytically stability, with 120 hours of cytotoxic activity. Similar results were obtained using human epithelial adenocarcinoma cells (Caco-2 cells).