Shirinzadeh Hanif, Ince Elif, Westwell Andrew D, Gurer-Orhan Hande, Suzen Sibel
a Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Erzincan University , Yalnizbag Yerleskesi , Erzincan , Turkey .
b Department of Pharmaceutical Toxicology , Faculty of Pharmacy, Ege University , Izmir , Turkey .
J Enzyme Inhib Med Chem. 2016 Dec;31(6):1312-21. doi: 10.3109/14756366.2015.1132209. Epub 2016 Jan 8.
Melatonin (MLT) is a well-known free-radical scavenger, involving in the prevention of cellular damage that can lead to cancer, ageing and a variety of neurodegenerative diseases. Research on MLT-related compounds has been required to optimise the maximum pharmaceutical activity with the lowest side effects. In our ongoing research, we have synthesized new indole-based MLT analogues as potential antioxidant agents by modifying the MLT molecule. In this study, we build on previous findings, through the synthesis, characterization and in vitro antioxidant profiling of a series of new indole-based MLT analogues which possess triazole, thiadiazole and carbothioamides on the third position on the indole ring. In vitro antioxidant activity was investigated by evaluating their reducing effect against oxidation of a redox sensitive fluorescent probe and their radical scavenging activity was assessed via the DPPH assay. In addition, in vitro cytotoxic effects of newly synthesized compounds were investigated in CHO-K1 cells using the MTT assay.
褪黑素（MLT）是一种著名的自由基清除剂，参与预防可能导致癌症、衰老和多种神经退行性疾病的细胞损伤。为了以最低的副作用优化最大的药物活性，需要对与MLT相关的化合物进行研究。在我们正在进行的研究中，我们通过修饰MLT分子，合成了新的基于吲哚的MLT类似物作为潜在的抗氧化剂。在本研究中，我们基于先前的发现，通过合成、表征以及对一系列在吲哚环第三位上具有三唑、噻二唑和碳硫酰胺的新型基于吲哚的MLT类似物进行体外抗氧化分析。通过评估它们对氧化还原敏感荧光探针氧化的还原作用来研究体外抗氧化活性，并通过DPPH测定法评估它们的自由基清除活性。此外，使用MTT测定法在CHO-K1细胞中研究了新合成化合物的体外细胞毒性作用。
