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新型有机硫属元素多靶点药物:硫属元素齐多夫定衍生物的合成及其抗氧化和抗肿瘤活性

New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives.

作者信息

de Souza Diego, Mariano Douglas O C, Nedel Fernanda, Schultze Eduarda, Campos Vinícius F, Seixas Fabiana, da Silva Rafael S, Munchen Taiana S, Ilha Vinicius, Dornelles Luciano, Braga Antonio L, Rocha João B T, Collares Tiago, Rodrigues Oscar E D

机构信息

†LabSelen-NanoBio - Departamento de Química, Universidade Federal de Santa Maria, 97105-900 Santa Maria, Brazil.

§Molecular and Cellular Oncology Group, Graduate Program in Biotechnology, Universidade Federal de Pelotas, 96010-610 Pelotas, Brazil.

出版信息

J Med Chem. 2015 Apr 23;58(8):3329-39. doi: 10.1021/jm5015296. Epub 2015 Apr 8.

Abstract

In this article we present the synthesis, characterization, and in vitro biological and biochemical activities of new chalcogenozidovudine derivatives as antioxidant (inhibition of TBARS in brain membranes and thiol peroxidase-like activity) as well as antitumoral agents in bladder carcinoma 5637. A prominent response was obtained for the selected chalcogenonucleosides, showing effective antioxidant and antitumoral activities.

摘要

在本文中,我们介绍了新型硫属元素代齐多夫定衍生物的合成、表征及其体外生物学和生物化学活性,这些衍生物具有抗氧化剂(抑制脑膜中的硫代巴比妥酸反应物和硫醇过氧化物酶样活性)以及膀胱癌5637中的抗肿瘤剂的作用。所选的硫属元素核苷获得了显著的反应,显示出有效的抗氧化和抗肿瘤活性。

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