2. Academic Validation
  3. Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles

Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles

  • Eur J Med Chem. 2014 May 22:79:273-81. doi: 10.1016/j.ejmech.2014.04.008.
Kathleen Santos 1,  Mafalda Laranjo 2,  Ana Margarida Abrantes 2,  Ana F Brito 3,  Cristina Gonçalves 4,  Ana Bela Sarmento Ribeiro 4,  M Filomena Botelho 2,  Maria I L Soares 5,  Andreia S R Oliveira 5,  Teresa M V D Pinho e Melo 6
Affiliations

Affiliations

  • 1 Biophysics Unit, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal.
  • 2 Biophysics Unit, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; CIMAGO - Center of Investigation in Environment, Genetics and Oncobiology, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; IBILI - Institute for Biomedical Imaging and Life Science, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal.
  • 3 Biophysics Unit, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; IBILI - Institute for Biomedical Imaging and Life Science, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal.
  • 4 CIMAGO - Center of Investigation in Environment, Genetics and Oncobiology, Faculty of Medicine of University of Coimbra, Azinhaga de Santa Comba, Celas, 3004-548 Coimbra, Portugal; Applied Molecular Biology, University Clinic of Haematology, Faculty of Medicine of University of Coimbra, Coimbra, Portugal.
  • 5 Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal.
  • 6 Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal. Electronic address: tmelo@ci.uc.pt.
PMID: 24747064 DOI: 10.1016/j.ejmech.2014.04.008
Abstract

Further studies on 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles as Anticancer agents against breast Cancer are reported, allowing to demonstrate the potential of these compounds for the therapy of the triple-negative breast Cancer, the most challenging tumors in clinical practice. These compounds were assayed for their in vitro cytotoxicity on several human breast Cancer cell lines (MCF7, HCC1954 and HCC1806 cell lines). Particularly interesting were the results obtained for 4-hydroxyphenyl substituted derivative, which proved to be the most promising compound regarding HCC1806 cell line, a triple-negative breast Cancer. The effects of the two most active compounds on cell survival, viability, cell cycle, DNA damage and expression of proteins related to cell death pathways were studied. The reported results consolidate the potential of 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles for the therapy of breast Cancer, particularly the triple-negative.

Keywords

6,7-Bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazole; Antitumor activity; Breast cancer; Triple-negative breast cancer.

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