Conjugation of a gold(iii) complex with vitamin B1 and chlorambucil derivatives: anticancer evaluation and mechanistic insights.,Metallomics

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Conjugation of a gold(iii) complex with vitamin B1 and chlorambucil derivatives: anticancer evaluation and mechanistic insights.
Metallomics ( IF 2.9 ) Pub Date : 2020-03-03 , DOI: 10.1039/c9mt00304e
Leila Tabrizi ₁ , Fatemeh Abyar

Affiliation

A novel cyclometalated gold(III) complex supported by chlorambucil coupled with phenylpyridine (CHL-N^C) and a hybrid of vitamin B1 with dithiocarbamate (B1-DTC) with the formula [(CHL-N^C)Au^III(B1-DTC)](Cl₂), 1, was synthesized and fully characterized using different techniques, including multinuclear NMR, mass spectrometry, and elemental analysis. This complex is water-soluble and stable in a biological environment. This new complex offers a new scaffold to explore the biological properties of gold(III) complexes as an anticancer drug. The antiproliferative activities of complex 1 and free ligands against breast and colon cancer cells showed auspicious results with IC₅₀ values in the micromolar range for complex 1 and more active than cisplatin and free ligands with selectivity over non-tumorigenic cells human lung fibroblasts, MRC-5. The DNA binding and inhibition of thioredoxin reductase of complex 1 were studied and compared with molecular docking results. Moreover, the Au cellular uptake and apoptosis of this new complex were investigated.

中文翻译：

金（iii）配合物与维生素B1和苯丁酸氮芥衍生物的缀合：抗癌评估和机理见解。

一种新型的环金属化的金（III）络合物，由苯丁环苄偶联苯基吡啶（CHL-N ^ C）以及维生素B1与二硫代氨基甲酸酯（B1-DTC）的杂物组成，其式[（CHL-N ^ C）Au ^III（B1-合成并使用多种技术（包括多核NMR，质谱和元素分析）对DTC）]（Cl ₂），1进行了全面表征。该复合物是水溶性的，并且在生物环境中稳定。这种新的复合物提供了一种新的支架，以探索作为抗癌药物的金（III）配合物的生物学特性。配合物1的抗增殖活性以及针对乳腺癌和结肠癌细胞的游离配体显示出了吉祥的结果，复合物1的IC ₅₀值在微摩尔范围内，比顺铂和游离配体更具活性，对非致瘤细胞人肺成纤维细胞MRC-5具有选择性。研究了配合物1的DNA结合和硫氧还蛋白还原酶的抑制作用，并与分子对接结果进行了比较。此外，研究了该新复合物的Au细胞摄取和凋亡。

更新日期：2020-03-03

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