5 years ago

Improve the anticancer potency of the platinum(II) complexes through functionalized leaving group

Improve the anticancer potency of the platinum(II) complexes through functionalized leaving group
Two platinum(II) complexes with 3,3-dimethoxycyclobutane-1,1-dicarboxylate as a leaving group were synthesized and spectrally characterized. In vitro cytotoxicity study on these complexes indicated that complex 2 showed considerable cytotoxicity against the tested cell lines. Notably, the higher antiproliferative activity of complex 2 relative to the corresponding parent compound [Pt(dach)(CBDCA)] demonstrated that the introduction of two methoxy groups in the 1,1-cyclobutanedicarboxylate (CBDCA) can improve the anticancer activity of the resulting platinum(II) complexes. Moreover, cellular accumulations of complexes 1 and 2 were slightly higher than those of their parent compounds carboplatin and Pt(dach)(CBDCA), respectively. Flow cytometry study revealed that complexes 1 and 2 produced death of tumor cells through an apoptotic pathway. Comparison of the chemical reactivity of Pt(dach)(CBDCA) and complex 2 with biologically relevant nucleophiles (l-Met and thiourea) via a kinetic method were studied by UV–Vis technique. The results showed that the reaction rates of complex 2 with nucleophiles were faster than that of Pt(dach)(CBDCA). DFT calculations showed that Pt(dach)(CBDCA) has slightly higher activation energies than complex 2 for the studied reactions. Overall, the introduction of two methoxy groups to the skeleton of 1,1-cyclobutanedicarboxylate can not only change the kinetic reactivity of the resulting platinum(II) complexes, but also enhance their anticancer efficacy.

Publisher URL: www.sciencedirect.com/science

DOI: S0162013417302921

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