Synthesis, Spectroscopic Characterization and in Vitro Cytotoxicity Assay of Mropholine Mannich Base Derivatives of Benzimidazole with Some Heavy Metals

M. Alias, S. Bakir
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引用次数: 4

Abstract

Mannich bases derivatives of Benzimidazole were prepared from condensation reaction of 2-mercaptobenzimidazole with formaldeyhed once with mropholine and another with pyrazinamide to prepare L1 and L2 respectively, coordinated with three metal ions of Pd(II), Pt(IV) and Au(III). The structures of these compounds were confirmed by metal and elemental analyses, UV-Vis and FT-IR spectroscopy, magnetic susceptibility, conductivity measurement at room temperature, 1HNMR and 13CNMR. Experimental results showed that the ligands (L1&L2) coordinated as bi-dentate and tridentate with metal ions respectively. Cytotoxicity of Mannich bases and their metal complexes were examined against mice cell line RAW 264.7 using MTT method .Each cell line was injected by following doses (400,200,100 and 50) µg/ml of prepared compounds by using mice cell as a negative control and cis-platin as a positive control. The ligands and Pd(II), Pt(IV), Au(III) complexes showed good activity at various concentrations especially Pd(II) complexes of both complexes.
含重金属苯并咪唑啉曼尼希碱衍生物的合成、光谱表征及体外细胞毒性测定
以2-巯基苯并咪唑与甲醛缩合为原料,分别与呋喃和吡嗪酰胺缩合为L1和L2,并与Pd(II)、Pt(IV)和Au(III)三种金属离子配位,制备了曼尼希碱类苯并咪唑衍生物。这些化合物的结构通过金属和元素分析、紫外-可见光谱和红外光谱、磁化率、室温电导率、1HNMR和13CNMR进行了证实。实验结果表明,配体(l1和l2)分别与金属离子呈双齿配位和三齿配位。采用MTT法检测曼尼希碱及其金属配合物对小鼠细胞系RAW 264.7的细胞毒性。以小鼠细胞为阴性对照,顺铂为阳性对照,分别以400,200,100和50µg/ml的剂量注射各细胞系。配体和Pd(II)、Pt(IV)、Au(III)配合物在不同浓度下均表现出良好的活性,尤其是两种配合物的Pd(II)配合物。
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