da Cruz, Eduardo H.G. ; Silvers, Molly A. ; Jardim, Guilherme A.M. ; Resende, Jarbas M. ; Cavalcanti, Bruno C. ; Bomfim, Igor S. ; Pessoa, Claudia ; de Simone, Carlos A. ; Botteselle, Giancarlo V. ; Braga, Antonio L. ; Nair, Divya K. ; Namboothiri, Irishi N.N. ; Boothman, David A. ; da Silva Júnior, Eufrânio N. (2016) Synthesis and antitumor activity of selenium-containing quinone-based triazoles possessing two redox centres, and their mechanistic insights European Journal of Medicinal Chemistry, 122 . pp. 1-16. ISSN 0223-5234
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Official URL: http://doi.org/10.1016/j.ejmech.2016.06.019
Related URL: http://dx.doi.org/10.1016/j.ejmech.2016.06.019
Abstract
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 IC50values < 0.3 μM. 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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | β-Lapachone; Quinone; Click Chemistry; Chalcogens; Selenium. |
| ID Code: | 121325 |
| Deposited On: | 14 Jul 2021 10:00 |
| Last Modified: | 14 Jul 2021 10:00 |
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