Department of Chemistry, Aligarh Muslim University, Aligarh 202002, Uttar Pradesh, India.
Spectrochim Acta A Mol Biomol Spectrosc. 2011 Jan;78(1):45-51. doi: 10.1016/j.saa.2010.06.009. Epub 2010 Jun 12.
Valine derived chiral complexes of SnCl4 (1) and ZrCl4 (2) were designed as potent antitumor agents. These complexes were characterized by elemental analysis, IR, 1H NMR, 119Sn NMR and ESI mass spectroscopy. In vitro binding studies of complexes 1 and 2 under physiological conditions at room temperature with CT-DNA were carried out employing UV-vis absorption titration, fluorescence studies and viscosity measurements. The extent of binding was quantified by Kb values of complexes 1 and 2 which were found to be 1.97×10(4) and 1.17×10(3) M(-1), respectively, suggesting that complex 1 has significantly greater DNA binding propensity in contrast to the complex 2. The mode of action at the molecular level was ascertained by the interaction of complex 1 with 5'GMP and 5'TMP which revealed that complex 1 binds via electrostatic mode with the oxygen of the negatively charged surface phosphate group of the DNA helix. The supercoiled pBR322 plasmid DNA cleavage activity of complex 1 was ascertained by gel electrophoresis assay.
以缬氨酸为配体合成的 SnCl4（1）和 ZrCl4（2）手性配合物被设计为有效的抗肿瘤试剂。通过元素分析、IR、1H NMR、119Sn NMR 和 ESI 质谱对这些配合物进行了表征。在室温生理条件下，通过紫外-可见吸收滴定、荧光研究和粘度测量，对配合物 1 和 2 与 CT-DNA 的体外结合研究进行了研究。通过 Kb 值定量了配合物 1 和 2 的结合程度，发现分别为 1.97×10(4)和 1.17×10(3) M(-1)，这表明配合物 1 与配合物 2 相比，具有更大的 DNA 结合倾向。通过配合物 1 与 5'GMP 和 5'TMP 的相互作用，确定了其在分子水平上的作用模式，表明配合物 1 通过静电模式与 DNA 螺旋中带负电荷的磷酸基团的氧结合。通过凝胶电泳分析确定了配合物 1 对超螺旋 pBR322 质粒 DNA 的切割活性。
