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Synthesis characterization and biological activities of imidazo12-apyridine based gold(III) metal complexes

机译:咪唑并12-a吡啶基金(III)金属配合物的合成表征和生物学活性

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摘要

Five imidazo [1,2-a]pyridine derivatives and their Au(III) complexes were synthesized. The compounds were characterized by 1H-NMR, 13C-NMR, IR, mass, UV-visible, elemental analysis, conductivity and magnetic measurement studies. All the compounds were screened for diverse biological activities to check the effect of coordination of Au(III) with imidazo [1,2-a]pyridine heterocycles. The DNA interaction ability of compounds were studied as the change in absorption maxima and position of HS-DNA in presence of compounds and viscosity measurement due to change in DNA length under the influence of compounds. The computational insight of compound-DNA interaction was taken in docking study. All the results suggest intercalation mode of binding. The cellular level cytotoxic nature of compounds was evaluated using trypan blue dye staining of dead cell in cell viability assay. The smearing of DNA was observed, while DNA extracted from S. pombe cells in presence of complexes was subjected to gel electrophoresis, which shows their toxic effect on DNA. The complexes were evaluated for cytotoxicity on human A549 (Lung adenocarcinoma) cell line by MTT assay (IC50 values). The in vitro cytotoxicity in terms of LC50 value was checked on a simple zoological organism, brine shrimp.
机译:合成了五个咪唑并[1,2-a]吡啶衍生物及其Au(III)配合物。通过 1 H-NMR, 13 C-NMR,IR,质量,紫外可见,元素分析,电导率和磁测量研究对其进行表征。筛选所有化合物的多种生物活性,以检查Au(III)与咪唑并[1,2-a]吡啶杂环的配位作用。研究化合物的DNA相互作用能力,包括存在化合物时HS-DNA的最大吸收量和位置的变化以及由于化合物作用下DNA长度的变化引起的粘度测量。化合物-DNA相互作用的计算见解被用于对接研究中。所有结果表明结合的嵌入模式。在细胞活力测定中使用死细胞的锥虫蓝染料染色来评估化合物的细胞水平细胞毒性性质。观察到DNA的涂片,而在复合物存在下从粟酒裂殖酵母细胞中提取的DNA进行了凝胶电泳,显示了它们对DNA的毒性作用。通过MTT测定法(IC50值)评价该复合物对人A549(肺腺癌)细胞系的细胞毒性。在LC50值方面,在简单的动物性生物盐水虾上检查了体外细胞毒性。

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