Synthesis, characterization and cytotoxicity of platinum(II)/palladium(II) complexes with 1,3-diaminopropane and 4-toluensulfonyl-l-amino acid dianion

Anions Models, Molecular Dose-Response Relationship, Drug Molecular Structure Antineoplastic Agents HL-60 Cells Diamines 01 natural sciences 0104 chemical sciences Tosyl Compounds Structure-Activity Relationship Cell Line, Tumor Organometallic Compounds Humans Amino Acids Drug Screening Assays, Antitumor Palladium Cell Proliferation Platinum
DOI: 10.1016/j.ejmech.2012.09.052 Publication Date: 2012-10-23T19:31:23Z
ABSTRACT
Eight novel platinum(II)/palladium(II) complexes with 1,3-dap and 4-toluensulfonyl-l-amino acid dianion, [Pt(1,3-dap)(TsalaNO)]·0.5H(2)O (1a), [Pt(1,3-dap)(TsvalNO)] (1b), [Pt(1,3-dap)(TspheNO)] (1c), [Pt(1,3-dap)(TsserNO)] (1d), [Pd(1,3-dap)(TsalaNO)]·1.5H(2)O (2a), [Pd(1,3-dap)(TsvalNO)] (2b), [Pd(1,3-dap)(TspheNO)] (2c) and [Pd(1,3-dap)(TsileNO)] (2d) have been synthesized and characterized by elemental analysis, IR, UV, (1)H NMR and mass spectrometry techniques. Crystal structure of the complex 1b has been determined by X-ray diffraction. The cytotoxicity was tested by MTT and SRB assays. The complexes (1a-1d and 2a-2d) exert cytotoxicity against Bel-7402, HL-60, KB and BGC-823, but none of them is more active than cisplatin. The results suggest that metal ions, amino acids and aliphatic N-containing ligands have effect on cytotoxicity, while the IC(50) values do not show definite correlation with variation of them.
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