有机锡(IV)N-乙基-N-苄基二硫代氨基甲酸酯配合物的开发:有机锡(IV)N-乙基-N-苄基二硫代氨基甲酸络合物的开发:关于其合成、表征及其对 A549 细胞系杀细胞作用的研究

IF 2.6 4区 医学 Q3 CHEMISTRY, MEDICINAL Anti-cancer agents in medicinal chemistry Pub Date : 2024-04-17 DOI:10.2174/0118715206309421240402093335
Nurul Amalina Abd Aziz, Normah Awang, Nurul Farahana Kamaludin, Nur Najmi Mohamad Anuar, Asmah Hamid, Kok Meng Chan, Suhana Arshad
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引用次数: 0

摘要

背景:二硫代氨基甲酸有机锡(IV)复合物在药物化学中非常重要,由于其独特的性质可增强靶向递送,因此在靶向癌细胞方面具有潜力。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盐复合物(ONBDCs),并评估其对 A549 细胞(常用作人类肺癌研究的模型)的细胞毒性。 背景:有机锡(IV)化合物是药物化学中的重要成分:有机锡(IV)化合物通过两种主要机制表现出强大的细胞毒性:通过外部磷酸基团与 DNA 结合,以及破坏内部磷脂代谢,这与顺铂的作用机制类似。此外,这些化合物独特的立体电子学特性赋予了它们非凡的治疗潜力。研究方法两种 ONBDC 衍生物--ONBDC 1(二甲基锡(IV)N-乙基-N-苄基二硫代氨基甲酸酯)和 ONBDC 2(三苯基锡(IV)N-乙基-N-苄基二硫代氨基甲酸酯)--是通过氯化锡(IV)与 N-乙基苄胺在二硫化碳存在下的反应合成的。研究人员采用了一系列分析技术,包括元素分析、红外光谱、核磁共振光谱、紫外可见光谱、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。采用 MTT 法评估了 ONBDCs 对 A549 细胞的细胞毒性作用。结果:成功合成了这两种化合物,并通过元素分析和光谱分析对其进行了表征。MTT 试验显示,ONBDC 2 对 A549 细胞具有显著的细胞毒性,IC50 值为 0.52 μM。此外,与市售化疗药物顺铂(IC50:32 μM)相比,ONBDC 2 对 A549 细胞株的细胞毒性活性明显更高:采用原位法合成了该化合物。然后,我们利用元素分析和光谱分析对化合物进行了表征。随后,利用 MTT 试验筛选了该化合物的细胞毒性潜力。结论因此,研究表明 ONBDC 2 具有重要的抗癌特性,应将其作为改良和专门治疗癌症的首选药物进行进一步研究。
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The Development of Organotin(IV) N-Ethyl-N-Benzyldithiocarbamate Complexes: A Study on Their Synthesis, Characterization, and Cytocidal Effects on A549 Cell Line
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. background: Organotin(IV) compounds exhibit potent cytotoxicity through two primary mechanisms: binding to DNA via external phosphate groups and disrupting internal phospholipid metabolism, similarly to the mechanism of action of cisplatin. Additionally, the distinct stereoelectronic properties of these compounds endow them with exceptional therapeutic potential. Method: 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). method: The compound was synthesized by using the in-situ method. Then, we used the elemental and spectroscopies analysis to characterize the compound. Subsequently, the cytotoxic potential of this compound is screened by using MTT assay. Conclusion: 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.
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来源期刊
Anti-cancer agents in medicinal chemistry
Anti-cancer agents in medicinal chemistry ONCOLOGY-CHEMISTRY, MEDICINAL
CiteScore
5.10
自引率
3.60%
发文量
323
审稿时长
4-8 weeks
期刊介绍: Formerly: Current Medicinal Chemistry - Anti-Cancer Agents. Anti-Cancer Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of anti-cancer agents. Each issue contains a series of timely in-depth reviews and guest edited issues written by leaders in the field covering a range of current topics in cancer medicinal chemistry. The journal only considers high quality research papers for publication. Anti-Cancer Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cancer drug discovery.
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