Abstract

A series of novel binuclear titanium (IV) complexes, [Ti(sal)L^I–V(OBu)(μ-OBu)]₂, was synthesized by the reaction of salicylic acid (H₂sal) and substituted indoles (L^I = Tryptophol, L^II = 5-Methoxyindole, L^III = Indole-5-Carboxaldehyde, L^IV = 5-Cyanoindole, L^V = 6-Nitroindole) with titanium(IV) tetrabutoxide in predetermined molar ratios under stirring and refluxing conditions in THF solvent. The chemical structure of synthesized complexes was found to be binuclear based on the FTIR, ^IH (proton) NMR and ESI-Mass (Electron-spray ionization) spectroscopic data. Each titanium metal was surrounded by two bridged butoxy groups and one terminal butoxy group along with bidentate salicylic acid and coordinated substituted indoles. These complexes were investigated for antioxidant potential using DPPH (2,2-diphenyl-1-picrylhydrazyl) assay where they exhibited moderate to good antioxidant activity. Gel electrophoresis method was employed to study the ct-DNA (calf thymus DNA) cleavage efficiency of complexes using an agarose gel. Antimicrobial results stated that most of the complexes were ineffective against selected bacterial and fungal strains. Complexes were investigated for anticancer activity against two selected cancerous cell lines (L6 and L929). From MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay, it has been inferred that complexes 1 and 2 have better anticancer properties than their respective indoles. The DNA binding study of synthesized complexes studied in order to check their efficacy to hinder DNA replication/transcription using electronic absorption and fluorescence spectroscopy revealed them as electrostatic/groove binder. The synthesized complexes were also evaluated for antidiabetic properties using alpha-amylase inhibition assay and complex 5 possessed better alpha-amylase inhibition activity than other complexes.

Graphic abstract

Synopsis: The synthesis, structural characterizationand biological activities of a novel binuclear titanium(IV) complexes [Ti(sal)L^I–V(OBu)(μ-OBu)]₂ is reported.

中文翻译：

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新型钛（IV）配合物的合成，表征，DNA结合和生物学研究

摘要

水杨酸（H ₂ sal）与取代的吲哚（L ^I）反应合成了一系列新型双核钛（IV）配合物[Ti（sal）L ^I–V（OBu）（μ-OBu）] ₂  =色醇，L ^II  = 5-甲氧基吲哚，L ^III  =吲哚-5-甲醛，L ^IV  = 5氰基吲哚，L ^V  = 6-硝基吲哚）与钛（IV），四丁氧基中的THF搅拌和回流条件下规定的摩尔比的溶剂。根据FTIR，^I发现合成的配合物的化学结构是双核的，H（质子）NMR和ESI-质谱（电子喷雾电离）光谱数据。每种钛金属都被两个桥接的丁氧基和一个末端的丁氧基以及二齿水杨酸和配位取代的吲哚所包围。使用DPPH（2,2-二苯基-1-吡啶并肼基）分析法研究了这些络合物的抗氧化潜力，这些化合物表现出中等至良好的抗氧化活性。使用琼脂糖凝胶，采用凝胶电泳法研究复合物的ct-DNA（小牛胸腺DNA）裂解效率。抗菌结果表明，大多数复合物对选定的细菌和真菌菌株均无效。研究了复合物对两种选定的癌细胞系（L6和L929）的抗癌活性。通过MTT（3-（4,5-二甲基噻唑-2-基）-2,5-二苯基溴化四唑）测定，1和2比它们各自的吲哚具有更好的抗癌性能。为了检查使用电子吸收和荧光光谱法检查其阻碍DNA复制/转录的功效，对合成的复合物进行了DNA结合研究，结果显示它们为静电/沟槽结合剂。还使用α-淀粉酶抑制试验评估了合成的复合物的抗糖尿病特性，并且复合物5具有比其他复合物更好的α-淀粉酶抑制活性。

图形摘要

简介：报道了一种新型双核钛（IV）配合物[Ti（sal）L ^I-V（OBu）（μ-OBu）] ₂的合成，结构表征和生物学活性。