Thiazole derivatives are recognized to possess various biological activities as antiparasitic, antifungal, antimicrobial and antiproliferative. The present work reports the synthesis of 22 new substances belonging to two classes of compounds: thiosemicarbazones and thiazoles, with the purpose of developing new drugs that present high specificity for tumor cells and low toxicity to the organism. A cytotoxic screening was performed to evaluate the performance of the new derivatives in five tumor cell lines. Eight compounds were shown to be promising in at least three tumor cell lines. These compounds had their IC₅₀ determined within 72 h and the activity structure ratio was assessed. The effect of the best compounds on PBMC and hemolytic activity assay was then evaluated. The compound 1d was considered the most promising among the samples tested and its influence on cell cycle, DNA fragmentation and mitochondrial depolarization was evaluated.

噻唑衍生物被认为具有多种生物活性，如抗寄生虫，抗真菌，抗微生物和抗增殖。本工作报道了属于两类化合物的22种新物质的合成：硫代半脲和噻唑，目的是开发对肿瘤细胞具有高特异性且对生物体毒性低的新药物。进行了细胞毒性筛选，以评估新衍生物在五种肿瘤细胞系中的性能。至少在三种肿瘤细胞系中，显示出八种化合物很有前途。这些化合物的IC ₅₀在72小时内确定，并评估了活性结构比。然后评估最佳化合物对PBMC的影响和溶血活性测定。化合物1d 被认为是最有希望的测试样本，并评估了其对细胞周期，DNA片段化和线粒体去极化的影响。