Departamento de Antibióticos, Centro de Biociências, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil.
Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil.
Eur J Med Chem. 2018 Jan 20;144:874-886. doi: 10.1016/j.ejmech.2017.12.040. Epub 2017 Dec 14.
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 IC 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、抗菌和抗增殖作用。本工作报道了属于两类化合物的 22 种新物质的合成：硫代缩氨基脲和噻唑，目的是开发对肿瘤细胞具有高特异性和对机体低毒性的新药。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。有 8 种化合物在至少三种肿瘤细胞系中表现出良好的效果。在 72 小时内确定了这些化合物的 IC 值，并评估了活性结构比。然后评估了最佳化合物对 PBMC 和溶血活性测定的影响。在所测试的样品中，化合物 1d 被认为是最有前途的，评估了其对细胞周期、DNA 片段化和线粒体去极化的影响。
