New substituted benzyl iminoether derivatives of the type cis- and trans-[PtCl2{E-N(H)=C(OMe)CH2-C6H4-p-R}(2)] (R = Me (1a, 2a), OMe (3a, 4a), F (5a, 6a)) have been synthesized and characterized by elemental analyses, FT-IR spectroscopy and NMR techniques. The iminoether ligands are in the E configuration, which is stable in solution and in the solid state, as confirmed by the H-1 NMR data. Complex trans-[PtCl2{E-N(H)=C(OMe)CH2-C6H4-p-F}(2)] (6a) was also characterized by an X-ray diffraction study. Complexes 1 a-6a have been tested against a panel of human tumor cell lines in order to evaluate their cytotoxic activity. cis-Isomers were significant more potent than the corresponding trans-isomers against all tumor cell lines tested; moreover, complexes la and 5a showed IC50 values from about 2-fold to 6-fold lower than those exhibited by cisplatin, used as reference platinum anticancer drug.

Synthesis, characterization and cytotoxic activity of substituted benzyl iminoether Pt(II) complexes of the type cis- and trans-[PtCl2{E-N(H)=C(OMe)CH2-C6H4-p-R}(2)] (R = Me, OMe, F). X-ray structure of trans-[PtCl2{E-N(H)=C(OMe)CH2-C6H4-p-F}(2)]

BETTIO, FRAZIA;MARZANO, CRISTINA;TASSAN, AUGUSTO;MOZZON, MIRTO;BERTANI, ROBERTA;MICHELIN, RINO
2008

Abstract

New substituted benzyl iminoether derivatives of the type cis- and trans-[PtCl2{E-N(H)=C(OMe)CH2-C6H4-p-R}(2)] (R = Me (1a, 2a), OMe (3a, 4a), F (5a, 6a)) have been synthesized and characterized by elemental analyses, FT-IR spectroscopy and NMR techniques. The iminoether ligands are in the E configuration, which is stable in solution and in the solid state, as confirmed by the H-1 NMR data. Complex trans-[PtCl2{E-N(H)=C(OMe)CH2-C6H4-p-F}(2)] (6a) was also characterized by an X-ray diffraction study. Complexes 1 a-6a have been tested against a panel of human tumor cell lines in order to evaluate their cytotoxic activity. cis-Isomers were significant more potent than the corresponding trans-isomers against all tumor cell lines tested; moreover, complexes la and 5a showed IC50 values from about 2-fold to 6-fold lower than those exhibited by cisplatin, used as reference platinum anticancer drug.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11577/2447040
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