New glutathione peroxidase mimetics-Insights into antioxidant and cytotoxic activity

New glutathione peroxidase mimetics-Insights into antioxidant and cytotoxic activity
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DOI:
10.1016/j.bmc.2016.10.018
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发表时间:
2017-01-01
影响因子:
3.5
通讯作者:
Scianowski, Jacek
Scianowski, Jacek
中科院分区:
医学3区
文献类型:
--
作者:
Pacula, Agata J.;Kaczor, Katarzyna B.;Scianowski, Jacek

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合成了一系列N-烷基苯并异硒唑-3(2 H)-酮,并用硼氢化钠还原得到相应的二硒醚。此外,还提出了碘酸钾氧化硒氮键形成的有效方法,观察到了二硒醚向苯并异硒唑酮的新转化。所有合成的衍生物的GPx样活性已通过NMR进行了评价。N-烯丙基二硒醚是比依布硒啉好五倍的抗氧化剂。还测试了对MCF 7和DU 145癌细胞的抗癌能力。N-环己基苯并异硒唑酮的抗增殖活性最高。(C)2016爱思唯尔有限公司版权所有。
A series of N-alkyl benzisoselenazol-3(2H)-ones has been obtained and transformed to corresponding diselenides by the reduction with sodium borohydride. Additionally, efficient methodology for the oxidative Se-N bond formation by potassium iodate has been presented, new conversion of diselenide to benzisoselenazolone was observed. The GPx-like activity of all synthetized derivatives has been evaluated by NMR. N-Allyl diselenide was up to five times better antioxidant than ebselen. Anticancer capacity towards MCF7 and DU145 cancer cells has been also tested. The highest antiproliferative activity was obtained for N-cyclohexyl benzisoselenazolone. (C) 2016 Elsevier Ltd. All rights reserved.