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Coluccia, M ; Nassi, A ; Boccarelli, A ; Giordano, D ; Cardellicchio, N ; Locker, D ; Leng, M ; Sivo, M ; Intini, FP ; Natile, G

In vitro and in vivo antitumour activity and cellular pharmacological properties of new platinum-iminoether complexes with different configuration at the iminoether ligands

Journal of Inorganic Biochemistry 77 (1-2) 31-35

par Administrateur - publié le

Abstract :

In order to widen our knowledge on antitumour trans-[PtCl2(iminoether)(2)] complexes, we have synthesised two new derivatives, trans[PtCl2(E-HN=C(OEt)Me)(2)] (1) and trarzs-[PtCl2(Z-HN=C(OEt)Me)(2)] (2), which differ in the configuration of the iminoether ligands. Isomer 1 showed an in vitro cytotoxicity similar to that of cisplatin in a panel of human tumour cell lines (mean IC50 = 8 and 7.7 mu M, respectively), whereas isomer 2 showed a lower activity (IC50 = 14.3 mu M). Both I and 2 isomers overcame cisplatin resistance of ovarian cancer cell line A2780/Cp8.