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. J Inorg Biochem. 2017 Jul 02;175:20-28 Authors: Zhao J, Wang D, Xu G, Gou S Abstract 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 ...
Source: Journal of Inorganic Biochemistry - Category: Biochemistry Authors: Tags: J Inorg Biochem Source Type: research

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