4.7 Article

Synthesis and biochemical studies of novel organic selenides with increased selectivity for hepatocellular carcinoma and breast adenocarcinoma

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 179, 期 -, 页码 515-526

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.06.075

关键词

Selenides; Diselenides; Selenocyanates; Hepatocellular carcinoma; Breast adenocarcinoma; Antioxidant; Michael-type reaction; Azo coupling

资金

  1. Deanship of Scientific Research, King Faisal University [186162]

向作者/读者索取更多资源

Nineteen organoselenides were synthesized and tested for their intrinsic cytotoxicity in hepatocellular carcinoma (HepG2) and breast adenocarcinoma (MCF-7) cell lines and their corresponding selective cytotoxicity (SI) was estimated using normal lung fibroblast (Wl-38) cells. Most of the organic selenides exhibited good anticancer activity, and this was more pronounced in HepG2 cells. Interestingly, the naphthoquinone- (5), thiazol- (12), and the azo-based (13) organic selenides demonstrated promising SI (up to 76). Furthermore, the amine 4c, naphthoquinone 5, and azo-based 13 and 15 organic selenides were able to down-regulate the expression of Bcl-2 and up-regulate the expression levels of IL-2, IL-6 and CD40 in HepG2 cells compared to untreated cells. Moreover, most of the synthesized candidates manifested good free radical-scavenging and GPx-like activities comparable to vitamin C and ebselen. The obtained results suggested that some of the presented organoselenium candidates have promising antiHepG2 and antioxidant activities. (C) 2019 Elsevier Masson SAS. All rights reserved.

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