Preparation and characterization of the new ligand 3,5-diacetyl-1,2,4-triazol bis(^(4)N-p-chlorophenylthiosemicarbazone),H_(5)L^(1),and its bimetallic complexes[Pd(μ-H_(3)L^(1))]_(2) and[Pt(μ-H_(3)L^(1))]_(2),are de...Preparation and characterization of the new ligand 3,5-diacetyl-1,2,4-triazol bis(^(4)N-p-chlorophenylthiosemicarbazone),H_(5)L^(1),and its bimetallic complexes[Pd(μ-H_(3)L^(1))]_(2) and[Pt(μ-H_(3)L^(1))]_(2),are described.The molecular structure of the complexes,determined by single crystal X-ray crystallography,reveals that each ligand coordinates,in an asymmetric dideprotonated form,to the metal ions in a square planar geometry.The new compounds synthesized have been evaluated for antiproliferative activity in vitro against NCI-H460,T-47D,A2780 and A2780cisR human cancer cell lines.The cytotoxicity data suggest that these compounds may be endowed with important antitumor properties,especially H_(5)L_(1),since they exhibit excellent antiproliferative activity surpassing the activity of cisplatin against three of the four tumor cell lines studied.The DNA binding ability of H5L1 and[Pt(μ-H_(3)L^(1))]_(2) with calf thymus DNA in Tris-HCl buffer solution(pH=7.2)was explored by UV-Vis absorption spectroscopy and viscosity measurements.These data indicated that both compounds bind to DNA by a groove binding mode.展开更多
基金Ministerio de Economía y Competitividad,Instituto de Salud Carlos III(PI1100659)of Spain for financial support.
文摘Preparation and characterization of the new ligand 3,5-diacetyl-1,2,4-triazol bis(^(4)N-p-chlorophenylthiosemicarbazone),H_(5)L^(1),and its bimetallic complexes[Pd(μ-H_(3)L^(1))]_(2) and[Pt(μ-H_(3)L^(1))]_(2),are described.The molecular structure of the complexes,determined by single crystal X-ray crystallography,reveals that each ligand coordinates,in an asymmetric dideprotonated form,to the metal ions in a square planar geometry.The new compounds synthesized have been evaluated for antiproliferative activity in vitro against NCI-H460,T-47D,A2780 and A2780cisR human cancer cell lines.The cytotoxicity data suggest that these compounds may be endowed with important antitumor properties,especially H_(5)L_(1),since they exhibit excellent antiproliferative activity surpassing the activity of cisplatin against three of the four tumor cell lines studied.The DNA binding ability of H5L1 and[Pt(μ-H_(3)L^(1))]_(2) with calf thymus DNA in Tris-HCl buffer solution(pH=7.2)was explored by UV-Vis absorption spectroscopy and viscosity measurements.These data indicated that both compounds bind to DNA by a groove binding mode.
