In Vitro Anticancer Evaluation of Platinum(II/IV) Complexes with Diisoamyl Ester of (S,S)-ethylenediamine-N,N’-di-2-propanoic Acid

摘要: Platinum(II) and platinum(IV) complexes [PtCln{(S,S)-(i-Am)2eddip}] (n = 2, 4: 1, respectively; (S,S)-(i-Am)2eddip O,O’-diisoamyl-(S,S)-ethylenediamine-N,N’-di-2-propanoate) were synthesized characterized by elemental analysis, IR, 1H 13C NMR spectroscopy mass spectrometry. Quantum chemical calculations used to predict formed isomers of 1 2. Furthermore, reduction 2 with ascorbic acid was followed time-dependant in order enable assignation the for complex 1. In vitro cytotoxic activity determined on a panel five human tumor cell lines derived from cervix adenocarcinoma (HeLa), alveolar basal (A549), breast (MDA-453), colorectal cancer (LS 174), erythromyeloblastoid leukemia (K562), as well one non-malignant lung fibroblast line (MRC-5), using MTT assay. Both exhibited high (2 against K562: IC50 5.4 µM), more active than cisplatin, moderate (1). caused considerable decrease number K562 cells G1, S G2 phases, concordantly increasing subpopulation sub-G1 fraction. Morphological analysis death induced platinum(II/IV) indicate apoptosis.