Abstract

New generation of copper(II) complexes with α-aminophosphonate as tridentate ligands has been synthesized. It is characterized by elemental analyses, spectral (IR, UV–Vis, MS, EPR, and 1H NMR) studies, thermal analysis as well as magnetic and molar conductance measurements. On the basis of spectral studies, a distorted square planar geometry has been assigned for all the complexes. Specific rotation measurements for both ligands and copper(II) complexes showed that they are enantiomerically enriched. The metal-free ligands and their Cu(II) complexes were tested for their in vitro anticancer activity against human colon carcinoma HT-29 cell lines. The results showed that the synthesized copper(II) complexes exhibited significantly higher anticancer activity than their free ligands. Among all the tested compounds in the series, the complex 5g demonstrated the highest anticancer activity at low micromolar inhibitory concentrations (IC50 = 14.2 µM) which is about a half of the reference drug activity, cisplatin (IC50 = 7.0 µM) in the same assay.

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