背景:二硫代氨基甲酸酯的有机锡(IV)配合物在药物化学中至关重要,由于其增强靶向递送的独特特性,在靶向癌细胞方面表现出潜力。本研究旨在合成和表征有机锡(IV)N-乙基-N-苄基二硫代氨基甲酸酯复合物(ONBDCs),并评估其对A549细胞的细胞毒性,它们通常被用作人类肺癌研究的模型。
方法:两种ONBDC衍生物-ONBDC1(二甲基锡(IV)N-乙基-N-苄基二硫代氨基甲酸酯)和ONBDC2(三苯基锡(IV)N-乙基-N-苄基二硫代氨基甲酸酯)-通过氯化锡(IV)与N-乙基苄基胺在二硫化碳存在下反应合成。一系列分析技术,包括元素分析,红外光谱,核磁共振波谱,紫外-可见光谱法,TGA/DTA分析,和X射线晶体学,对这些化合物进行了全面的表征。用MTT法评价ONBDCs对A549细胞的细胞毒作用。
结果:两种化合物均已合成并通过元素和光谱分析成功表征。MTT实验显示ONBDC2对A549细胞具有显著的细胞毒性,IC50值为0.52μM。此外,与市售化疗剂顺铂相比,ONBDC2对A549细胞系显示出明显更高的细胞毒性活性(IC50:32μM)。
结论:因此,研究表明,ONBDC2可能具有重要的抗癌特性,作为创造改良和专业化癌症治疗的顶级竞争者,应进一步加以探讨.
BACKGROUND: Organotin(IV) complexes of dithiocarbamate are vital in medicinal chemistry, exhibiting potential in targeting cancer cells due to their unique properties that enhance targeted delivery. This
study aimed to synthesize and characterize organotin(IV) N-ethyl-N-benzyldithiocarbamate complexes (ONBDCs) and evaluate their cytotoxicity against A549 cells, which are commonly used as a model for human lung cancer research.
METHODS: The two ONBDC derivatives - ONBDC 1 (dimethyltin(IV) N-ethyl-N-benzyldithiocarbamate) and ONBDC 2 (triphenyltin(IV) N-ethyl-N-benzyldithiocarbamate) - were synthesized via the reaction of tin(IV) chloride with N-ethylbenzylamine in the presence of carbon disulfide. A range of analytical techniques, including
elemental analysis, IR spectroscopy, NMR spectroscopy, UV-Vis spectrometry, TGA/DTA analysis, and X-ray crystallography, was conducted to characterize these compounds comprehensively. The cytotoxic effects of ONBDCs against A549 cells were evaluated using MTT assay.
RESULTS: Both compounds were synthesized and characterized successfully via
elemental and spectroscopies analysis. MTT assay revealed that ONBDC 2 demonstrated remarkable cytotoxicity towards A549 cells, with an IC50 value of 0.52 μM. Additionally, ONBDC 2 displayed significantly higher cytotoxic activity against the A549 cell line when compared to the commercially available chemotherapeutic agent cisplatin (IC50: 32 μM).
CONCLUSIONS: Thus, it was shown that ONBDC 2 could have important anticancer properties and should be further explored as a top contender for creating improved and specialized cancer treatments.