Synthesis, characterization and biological activity of new cyclometallated platinum(IV) complexes containing a para-tolyl ligand

作者: Mònica Solé , Cristina Balcells , Margarita Crespo , Josefina Quirante , Josefa Badia

DOI: 10.1039/C8DT01124A

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摘要: The synthesis of three new cyclometallated platinum(II) compounds containing a para-tolyl ligand and tridentate [C,N,N′] (cm1) or bidentate [C,N] an additional such as SEt2 (cm2) PPh3 (cm3) is reported. X-ray molecular structure compound cm3 also presented. Intermolecular oxidative addition methyl iodide iodine upon cm1, cm2 produced six novel platinum(IV) compounds. cytotoxic activity against panel human adenocarcinoma cell lines (A-549 lung, MDA-MB-231 MCF-7 breast, HCT-116 colon), DNA interaction, topoisomerase I, IIα, cathepsin B inhibition, cycle arrest, apoptosis ROS generation the investigated complexes are best results for antiproliferative were obtained cm1MeI cm1I2 arising from iodine, respectively, to cm1. Cyclometallated cm3MeI induce significant changes in mobility and, addition, cm1MeI, cm1I2, showed considerable IIα inhibitory activity. Moreover, exhibiting higher (cm1MeI cm1I2) found generate supress colon cancer growth by mixture arrest induction. 1H NMR experiments carried out buffered aqueous medium (pH 7.40) indicate that not reduced common biologically relevant reducing agents ascorbic acid, glutathione cysteine.

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