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Interaction of chromium(III) complex of chiral binaphthyl tetradentate ligand with DNA

机译:手性双萘四齿配体铬(III)配合物与DNA的相互作用

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摘要

Since conformation of the molecule plays a vital role in the activity of drug, we have investigated the DNA interaction of a chromium(III) complex with ligands in two conformations. Chromium(III) complexes derived from chiral binaphthyl Schiff base ligands, viz. R- and S-2,2'-bis(salicylideneamino) 1,1'-binaphthyl, have been synthesized and characterized by mass, IR, and electronic spectra. The interaction of these R- and S-binaphthyl Schiff base chromium(III) complexes with CT-DNA was investigated with the goal of examining whether the chirality has an influence on the chromium(III)-DNA binding properties. The difference in chirality of the ligand did not show any striking difference in binding properties. The binding constants for R and S conformers were estimated to be 18 (± 0.4) x 10~3 and 9.4 (± 0.3) x 10~3 M~(-1), respectively, through spectroscopic titrations. All the experimental results are suggestive that both the isomers are DNA groove binders. The results of steady-state as well as time-resolved fluorescence experiments, however, suggest that the R conformer has restricted mobility when bound to DNA because it is more deeply buried in the groove of DNA compared to the S isomer.
机译:由于分子的构象在药物活性中起着至关重要的作用,因此我们研究了铬(III)配合物与配体在两种构象中的DNA相互作用。衍生自手性联萘席夫碱配体的铬(III)配合物。 R-和S-2,2'-双(水杨亚氨基)1,1'-联萘已合成,并通过质谱,红外光谱和电子光谱表征。研究了这些R-和S-联萘基席夫碱铬(III)配合物与CT-DNA的相互作用,目的是检查手性是否对铬(III)-DNA结合特性有影响。配体的手性上的差异在结合特性上未显示任何显着差异。通过光谱滴定,R和S构象异构体的结合常数估计分别为18(±0.4)x 10〜3和9.4(±0.3)x 10〜3 M〜(-1)。所有的实验结果都表明这两种异构体都是DNA沟结合剂。但是,稳态和时间分辨荧光实验的结果表明,与S异构体相比,R构象异构体与DNA结合时具有受限的迁移率,因为它更深地埋在DNA的凹槽中。

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