2. Academic Validation
  3. Synthesis and evaluation of quinonoid compounds against tumor cell lines

Synthesis and evaluation of quinonoid compounds against tumor cell lines

  • Eur J Med Chem. 2011 Jan;46(1):399-410. doi: 10.1016/j.ejmech.2010.11.006.
Eufrânio N da Silva Jr 1,  Bruno C Cavalcanti,  Tiago T Guimarães,  Maria do Carmo F R Pinto,  Igor O Cabral,  Cláudia Pessoa,  Letícia V Costa-Lotufo,  Manoel O de Moraes,  Carlos K Z de Andrade,  Marcelo R Dos Santos,  Carlos A de Simone,  Marilia O F Goulart,  Antonio V Pinto
Affiliations

Affiliation

  • 1 Núcleo de Pesquisas de Produtos Naturais, UFRJ, 21941-971, Rio de Janeiro, RJ, Brazil. eufranio.junior@yahoo.com.br
PMID: 21115213 DOI: 10.1016/j.ejmech.2010.11.006
Abstract

Thirty two compounds were synthesized in moderate to high yields and showed activity against Cancer cells HL-60 (leukemia), MDA-MB435 (melanoma), HCT-8 (colon) and SF295 (central nervous system), with IC(50) below 2 μM for some compounds. The β-lapachone-based 1,2,3-triazoles showed the best cytoxicity profile and emerge as promising Anticancer prototypes. Insights about the Reactive Oxygen Species (ROS) mechanism of Anticancer action for some compounds were obtained by addition of 1-bromoheptane that deplete reduced glutathione (GSH) content and by using N-acetylcysteine that protects cells against apoptotic cellular death, as well by analysis of thiobarbituric acid reactive substances (TBARS) formation, and oxidative DNA damage after treatment detected by the comet assay with the Bacterial enzymes formamidopyrimidine DNA-glycosylase (FPG) and Endonuclease III (ENDOIII).

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