Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 122, Issue -, Pages 1-16Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.06.019
Keywords
beta-Lapachone; Quinone; Click chemistry; Chalcogens; Selenium
Categories
Funding
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico [480719/2012-8, PVE 401193/2014-4, 449348/2014-8, 474797/2013-9, 454171/2014-5]
- NIH/NCI [CA102792]
Ask authors/readers for more resources
Selenium-containing quinone-based 1,2,3-triazoles were synthesized using click chemistry, the copper catalyzed azide-alkyne 1,3-dipolar cycloaddition, and evaluated against six types of cancer cell lines: HL-60 (human promyelocytic leukemia cells), HCT-116 (human colon carcinoma cells), PC3 (human prostate cells), SF295 (human glioblastoma cells), MDA-MB-435 (melanoma cells) and OVCAR-8 (human ovarian carcinoma cells). Some compounds showed IC50 values < 0.3 mu M. The cytotoxic potential of the quinones evaluated was also assayed using non-tumor cells, exemplified by peripheral blood mononuclear (PBMC), V79 and L929 cells. Mechanistic role for NAD(P)H:Quinone Oxidoreductase 1 (NQO1) was also elucidated. These compounds could provide promising new lead derivatives for more potent anticancer drug development and delivery, and represent one of the most active classes of lapachones reported. (C) 2016 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available