Abstract：
A set of novels 2-thiohydantoin derivatives were synthesized and enaminone function was discussed at position 5 using DMFDMA catalyst which result in formation of pyrazole, isoxazole, benzoxazepine by using reagents such as hydrazine, hydroxylamine and 2-aminothiophenol. These newly synthesized compounds were evaluated for their antioxidant and antiproliferative activity. In vitro studies on the effect of 2-thiohydantoin on scavenging 2,2-diphenyl-1-picrylhydrazyl radical (DPPH•) confirmed the free radical scavenging and antioxidant activity of 2-thiohydantoin. The synthesized compounds show significant antioxidant activity. The in vitro antitumor activity of 2-thiohydantoin on MCF7 (breast) and PC3 cells (prostate) was evaluated using MTT assay. Some of the synthesized compounds show significant to moderate antiproliferative properties compared to reference drug erlotinib. Among all, compound 4a exhibit potent antitumor properties against MCF7 and PC3 cancer cell lines with IC50 = 2.53 ± 0.09 /ml & with IC50 = 3.25 ± 0.12 µg/ml respectively and has potent antioxidant activity with IC50 = 10.04 ± 0.49 µg/ml.
摘要：
合成了一组新颖的2-硫代乙内酰脲衍生物，并使用DMFDMA催化剂在5位讨论了烯胺酮功能，从而形成吡唑，异恶唑,通过使用肼等试剂，羟胺和2-氨基苯硫酚。评估了这些新合成的化合物的抗氧化和抗增殖活性。关于2-硫代乙内酰脲对2,2-二苯基-1-吡啶酰肼自由基（DPPH•）的清除作用的体外研究证实了2-硫代乙内酰脲的自由基清除和抗氧化活性。合成的化合物显示出显著的抗氧化活性。使用MTT测定法评估2-硫代乙内酰脲对MCF7（乳腺）和PC3细胞（前列腺）的体外抗肿瘤活性。与参比药物埃罗替尼相比,一些合成的化合物显示出显著至中等的抗增殖性质。其中,化合物4a对MCF7和PC3癌细胞具有有效的抗肿瘤特性，IC50=2.53±0.09/ml和IC50=3.25±0.12µg/ml，具有有效的抗氧化活性，IC50=10.04±0.49µg/ml。
