期刊
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
卷 16, 期 5, 页码 621-632出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520615666150916092035
关键词
Anticancer; diselenides; diversity-oriented synthesis (DOS); glutathione peroxidase mimics; isocyanide-based multicomponent reactions (IMCR); pseudopeptides; selenium-based quinones; Ugi reaction
资金
- Egyptian Ministry of Higher Education, Deutscher Akademischer Austauschdienst (DAAD)
- Leibniz Institute of Plant Biochemistry
- Mansoura University
An efficient route towards the synthesis of symmetrical diselenide and selenium-containing quinone pseudopeptides via one-pot Ugi and sequential nucleophilic substitution (S-N) methodology was developed. Compounds were evaluated for their antimicrobial and anticancer activities and their corresponding antioxidant/pro-oxidant profiles were assesed employing 2,2-diphenyl-1-picrylhydrazyl (DPPH), bleomycin dependent DNA damage and glutathione peroxidase (GPx)-like activity assays. Selenium based quinones were among the most potent cytotoxic compounds with a slight preference for MCF-7 compared to HepG2 cells and good free radical scavenging activity. Furthermore, symmetrical diselenides exhibited the most potent GPx-like activity compared to ebselen. Moreover, compounds 7, 8, 9 and 10 exhibited similar antifungal activity to the antifungal drug clotrimazole with modest activity against the Gram-positive bacterium S. aureus. These results indicate that some of the synthesized organoselenides are redox modulating agent with promising anti-cancer and antifungal potentials.
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