Metallo - Bioactive Compounds as Potential Novel Anticancer Therapy

Abstract

Mono and bi-organometallic complexes of Cu(II), Ni(II), Mn(II), Zn(II) and Ag(I) complexes with oxaloamide ligand has much potential as therapeutic and diagnostic agents. The ligand allows the thermodynamic and kinetic reactivity of the metal ion to be controlled and also provide a scaffold for functionalization. Specific examples involving the design of metal complexes as anticancer agents are discussed. These complexes have been synthesized and characterized by (1H-NMR, mass, IR, UV-VIS, ESR) spectra, magnetic moments and conductance measurements, elemental and thermal analyses. Molar conductances in DMF solution indicates that, the complexes are non-electrolytes. The ESR spectra of solid Cu(II) complexes (2-5) show an axial type indicating a d(X2-y2) ground state with a significant covalent bond character. However, Mn(II) complex(9), shows an isotropic type indicating an octahedral geometry. Cytotoxic evolution IC50 of the ligand and its complexes have been carried out. Cu(II) Complexes

Benzoxazole-based Zn(II) and Cu(II) Complexes Overcome Multidrug-resistance in Cancer

“…Thus, the three parent ligands 1-3 showed no obvious MDR-modulating activity, while complexes 4-6 displayed a remarkable inhibition of MDR, indicating that ligand coordination plays an important role in the active complexes. Such increased activity of the metal complexes can be explained on the basis of the Overtone concept and Tweedy chelation theory (37)(38)(39)(40)(41). It is important to note that ABC transporters are primary efflux pumps deriving their energy from the hydrolysis of ATP.…”