摘要 已经进行了钌 (II) 腙络合物 [RuCl(CO)(PPh3)2L](其中 L = 腙配体)的合成、光谱表征和生物学研究。腙是具有O和N作为供体的一元双齿配体,并且优选在所有配合物中以烯醇形式存在。配体HL1、HL2和HL3的分子结构由单晶X射线衍射确定。配体和复合物的 DNA 结合研究通过吸收光谱和粘度测量进行。结果表明,配体和复合物通过嵌入与 DNA 结合。通过凝胶电泳测定评估复合物的 DNA 切割活性,表明复合物是良好的 DNA 切割剂。针对 DPPH、OH、和 NO 自由基,表明配合物具有很强的自由基清除能力。此外,复合物对 HeLa 和 MCF-7 癌细胞系的体外细胞毒作用表明,复合物表现出显着的抗癌活性。
Mechanistic differences between in vitro assays for hydrazone-based small molecule inhibitors of anthrax lethal factor
作者:M. Leslie Hanna、Theodore M. Tarasow、Julie Perkins
DOI:10.1016/j.bioorg.2006.07.004
日期:2007.2
A systematically generated series of hydrazones were analyzed as potential inhibitors of anthrax lethal factor. The hydrazones were screened using one UV-based and two fluorescence-based in vitro assays. The study identified several inhibitors with IC50 values in the micromolar range, and importantly, significant differences in the types of inhibition were observed with the different assays. (c) 2006 Elsevier Inc. All rights reserved.
Synthesis, characterization, DNA binding, DNA cleavage, antioxidant and <i>in vitro</i> cytotoxicity studies of ruthenium(II) complexes containing hydrazone ligands
biological studies of ruthenium(II) hydrazone complexes [RuCl(CO)(PPh3)2L] (where L = hydrazone ligands) have been carried out. The hydrazones are monobasic bidentate ligands with O and N as the donors and are preferably found in the enol form in all the complexes. The molecular structure of the ligands HL1, HL2, and HL3 were determined by single-crystal X-ray diffraction. The DNA binding studies of the
摘要 已经进行了钌 (II) 腙络合物 [RuCl(CO)(PPh3)2L](其中 L = 腙配体)的合成、光谱表征和生物学研究。腙是具有O和N作为供体的一元双齿配体,并且优选在所有配合物中以烯醇形式存在。配体HL1、HL2和HL3的分子结构由单晶X射线衍射确定。配体和复合物的 DNA 结合研究通过吸收光谱和粘度测量进行。结果表明,配体和复合物通过嵌入与 DNA 结合。通过凝胶电泳测定评估复合物的 DNA 切割活性,表明复合物是良好的 DNA 切割剂。针对 DPPH、OH、和 NO 自由基,表明配合物具有很强的自由基清除能力。此外,复合物对 HeLa 和 MCF-7 癌细胞系的体外细胞毒作用表明,复合物表现出显着的抗癌活性。
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