2. Academic Validation
  3. It takes two to tango: synthesis of cytotoxic quinones containing two redox active centers with potential antitumor activity

It takes two to tango: synthesis of cytotoxic quinones containing two redox active centers with potential antitumor activity

  • RSC Med Chem. 2021 Aug 12;12(10):1709-1721. doi: 10.1039/d1md00168j.
Daisy J B Lima 1 2,  Renata G Almeida 3,  Guilherme A M Jardim 3 4,  Breno P A Barbosa 2 3,  Augusto C C Santos 3,  Wagner O Valença 3,  Marcos R Scheide 4,  Claudia C Gatto 5,  Guilherme G C de Carvalho 1,  Pedro M S Costa 1,  Claudia Pessoa 1,  Cynthia L M Pereira 3,  Claus Jacob 2,  Antonio L Braga 4,  Eufrânio N da Silva Júnior 3
Affiliations

Affiliations

  • 1 Department of Physiology and Pharmacology, Federal University of Ceará Fortaleza 60430-270 Ceará Brazil.
  • 2 Division of Bioorganic Chemistry, School of Pharmacy, University of Saarland 66123 Saarbruecken Germany.
  • 3 Institute of Exact Sciences, Department of Chemistry, Federal University of Minas Gerais Belo Horizonte 31270-901 Minas Gerais Brazil eufranio@ufmg.br.
  • 4 Department of Chemistry, Federal University of Santa Catarina Florianópolis Santa Catarina 88040-900 Brazil braga.antonio@ufsc.br.
  • 5 Institute of Chemistry, University of Brasilia Brasilia 70904-970 DF Brazil.
PMID: 34778772 DOI: 10.1039/d1md00168j
Abstract

We report the synthesis of 47 new quinone-based derivatives via Click Chemistry and their subsequent evaluation against Cancer cell lines and the control L929 murine fibroblast cell line. These compounds combine two redox centers, such as an ortho-quinone/para-quinone or Quinones/selenium with the 1,2,3-triazole nucleus. Several of these compounds present IC50 values below 0.5 μM in Cancer cell lines with significantly lower cytotoxicity in the control cell line L929 and good selectivity index. Hence, our study confirms the use of a complete and very diverse range of quinone compounds with potential application against certain Cancer cell lines.

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