Abstract |
The reaction of cis-[PtCl2(Me-2(S) under barO)(2)] with 1 equiv. of each of the amidoximes RC(NH2)=NOH in neutral media in MeOH results in the formation of compLexes cis-[PtO2\RC(NH2)=NOH\(Me-2(S) under barO)] (5 examples; 83-98\% isolated yieLds). In the presence of 2 equiv. of NaOH in MeOH solution, the reaction of cis-[PtCl2(Me2SO)(2)] with 1 equiv. of each of the amidoximes RC(NH2)=NOH Leads to [Pt\RC((N) under barH)=N (O) under bar\(Me-2(S) under baro)(2)] (7 examples; 74-95\% isoLated yieLds). ALL new compLexes were characterized by C, H, and N elemental analyses, HRESI+-MS, IR, H-1, C-13\H-1\, and CP-MAS TOSS C-13\H-1\ NMR spectroscopies, and additionally by single-crystal XRD (for seven species). The cytotoxic potency of six compounds was determined in the human cancer cell Lines CH1/PA-1, A549, SK -BR -3, and SW480. Generally, the second class of compLexes containing chelating amidoximato Ligands shows much higher cytotoxicity than the non-cheLate amidoxime analogs, despite the Lack of easily exchangeable chLorido Ligands. Especially, the complex [Pt(p-CF3C6H4C((N) under barH)=NO)(Me-2(S) under barO)(2)] displays a remarkable activity in the inherently cisplatin resistant SW480 cell Line (0.51 mu M vs. 3.3 mu M). |