2. Academic Validation
  3. 2H-1,2,3-Triazole-chalcones as novel cytotoxic agents against prostate cancer

2H-1,2,3-Triazole-chalcones as novel cytotoxic agents against prostate cancer

  • Bioorg Med Chem Lett. 2020 Oct 1;30(19):127454. doi: 10.1016/j.bmcl.2020.127454.
Sergio Pinheiro 1,  Jaqueline C Pessôa 2,  Erick M C Pinheiro 3,  Estela M F Muri 3,  Eclair Venturini Filho 4,  Laiza B Loureiro 4,  Maria Clara R Freitas 5,  Carlos M D Silva Junior 2,  Rodolfo G Fiorot 2,  José Walkimar M Carneiro 2,  Karina M Rotamiro 6,  Anderson R A Guimarães 7,  Karin J P Rocha-Brito 7,  Sandro J Greco 8
Affiliations

Affiliations

  • 1 Chemistry Institute, Fluminense Federal University, Outeiro de S. João Batista s/n, Centro, 24020-141 Niterói, RJ, Brazil. Electronic address: spinuff@gmail.com.
  • 2 Chemistry Institute, Fluminense Federal University, Outeiro de S. João Batista s/n, Centro, 24020-141 Niterói, RJ, Brazil.
  • 3 Department of Pharmaceutical Technology, Faculty of Pharmacy, Fluminense Federal University, Niterói, RJ, Brazil.
  • 4 Department of Chemistry, Espírito Santo Federal University, Av. Fernando Ferrari 514, Goiabeiras, 29075-910 Vitória, ES, Brazil.
  • 5 Department of Chemistry, Rio de Janeiro Rural Federal University, Seropédica, RJ, Brazil.
  • 6 Laboratory of Technological Innovation in Drugs and Cosmetics Development, State University of Maringá, Maringá, PR, Brazil.
  • 7 Department of Medicine, University Center of Maringá, Maringá, PR, Brazil.
  • 8 Department of Chemistry, Espírito Santo Federal University, Av. Fernando Ferrari 514, Goiabeiras, 29075-910 Vitória, ES, Brazil. Electronic address: grecosj@outlook.com.
PMID: 32736078 DOI: 10.1016/j.bmcl.2020.127454
Abstract

Prostate Cancer is an important cause of death in the male population and for which there is no satisfactory chemotherapy. Herein a new series of chalcone hybrids containing 2H-1,2,3-triazole core as the ring B has been synthesized and evaluated in vitro against PC-3 prostate Cancer cell line. Compounds 4a, 4c and 4e significantly reduced cell viability and showed IC50 of 28.55, 15.64 and 25.56 µM, respectively. The structure-activity relationship supported by computational chemistry points that the polarity of the molecular surface area should have some relevance to the efficiency of the compounds, in particular the ratio of the partial positive charge sites and the total molecular surface area exposed to the cell environment.

Keywords

1,2,3-Triazole; Chalcone; Endocrine cancer; Hybridization; Prostate cancer.

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