Pyrazle constituents have garnered consideration mainly because of their presumed biological and curative properties. Therefore, the goal of the presented research is to create some novel pyrazole-1-carbothiohydrazide derivatives with predicted biological functions using an accessible one-pot synthesis employing 3,5-dimethyl-1H-pyrazole-1-carbothiohydrazide (1) as a facile antecedent. The component 1 and 1,3-diphenylpropane-1,3-dione (2) interacted resulting in pyrazole derivative 3 when ethanol or acetic acid were supplied. However, when the substance 1 interacted in ethanol with either 2 or acetyl acetone 5, using the catalytic proportion of triethylamine offered, it yielded compounds 4 and 6 respectively. Ingredient 1 was subjected to additional reactions with ethyl cyanoacetate (7), stearic acid 10, or equivalent carboxylic acids 12a-c, resulted in the formation of 9, 11, and 13a-c consequently. Additionally, when 1 was combined with α-haloketones 14 or 16, it yielded the corresponding 1,3,4-thiadiazine derivatives, 15 and 17. Every designed product's chemical structure was established according to spectroscopic and analytical results. The cytotoxic activities of the synthesized chemicals were assessed against two carcinoma cell lines, and compared to the standard drug Cisplatin using the colorimetric MTT assay. Furthermore, the results revealed that chemical 17 was the most active against the liver and lung carcinoma cell lines giving potent IC50 value of 5.35 and 8.74 μM, respectively, compared with reference drug cisplatin (3.78 and 6.39 μM). Interestingly, ingredient 17 when evaluated for their toxicity against normal lung fibroblast (MRC-5) cells exhibited low toxic effects indicating the safe use. Generally, our results exerted promising bioactive compounds.

中文翻译：

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新型3,5-二甲基-1H-吡唑-1-硫代硫酰肼衍生物的便捷一锅合成和生物学评价作为新型抗肝癌（HepG2）和肺癌（A549）细胞系的抗肿瘤药物

吡唑成分之所以引起人们的关注，主要是因为它们的生物学和治疗特性。因此，本研究的目标是使用 3,5-二甲基-1H-吡唑-1-硫代酰肼 (1) 作为简便的一锅法合成，创造一些具有预测生物功能的新型吡唑-1-硫代硫酰肼衍生物。前因。当供给乙醇或乙酸时，组分1和1,3-二苯基丙烷-1,3-二酮(2)相互作用产生吡唑衍生物3。然而，当物质 1 在乙醇中与 2 或乙酰丙酮 5 相互作用时，利用所提供的三乙胺的催化比例，分别产生化合物 4 和 6。成分 1 与氰基乙酸乙酯 (7)、硬脂酸 10 或等效羧酸 12a-c 进行额外反应，最终形成 9、11 和 13a-c。此外，当1与α-卤代酮14或16结合时，得到相应的1,3,4-噻二嗪衍生物15和17。根据光谱和分析结果确定了每个设计产品的化学结构。针对两种癌细胞系评估了合成化学物质的细胞毒性活性，并使用比色 MTT 测定法与标准药物顺铂进行比较。此外，结果显示，与参考药物顺铂（3.78 和 6.39 μM）相比，化学物质 17 对肝癌和肺癌细胞系最有活性，其有效 IC50 值分别为 5.35 和 8.74 μM。有趣的是，在评估成分 17 对正常肺成纤维细胞 (MRC-5) 的毒性时，其毒性作用较低，表明可以安全使用。总的来说，我们的结果显示出有前景的生物活性化合物。