Cytotoxic Rhodium(III) Polypyridyl Complexes Containing the Tris(pyrazolyl)methane Coligand: Synthesis, DNA Binding Properties and Structure–Activity Relationships
作者:Ruth Bieda、Ingo Ott、Ronald Gust、William S. Sheldrick
DOI:10.1002/ejic.200900373
日期:2009.9
(1, 2) cytotoxicity. X-ray structural analyses of [RhCl(bpy)(tpm)][PF6]24 and [RhCl(phen)(tpm)][PF6]26 were performed, and the interaction of complexes 4–9 with DNA was investigated by CD and UV/Vis spectroscopy and by gel electrophoresis. CD and viscosity studies confirm strong intercalation of dppz complex 9 into DNA. Complexes 8 and particularly 9 (IC50 = 0.43, 0.37 μM) are potent cytotoxic agents
[RhCl(pp)(tpm)]2+ [pp = bpy, bpm, phen, tap, dpq, dppz] 4–9 类型的 RhIII 配合物是通过逐步处理 RhCl3·3H2O 或 mer,cis- [RhCl3(DMSO-κS)2(DMSO-κO)] 带有适当的多吡啶基配体 (pp),然后是三足配体三(吡唑基)甲烷 (tpm)。[RhCl3(CH3OH)(pp)] 1-3 类型的中间体,pp = bpy、phen、dpq 也被表征,但表现出低 (3) 或没有 (1, 2) 细胞毒性。对 [RhCl(bpy)(tpm)][PF6]24 和 [RhCl(phen)(tpm)][PF6]26 进行了 X 射线结构分析,并通过 CD 研究了复合物 4-9 与 DNA 的相互作用和紫外/可见光谱和凝胶电泳。CD 和粘度研究证实 dppz 复合物 9 强烈嵌入 DNA。复合物 8,尤其是 9 (IC50