Literature DB >> 24747064

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

Kathleen Santos1, Mafalda Laranjo2, Ana Margarida Abrantes2, Ana F Brito3, Cristina Gonçalves4, Ana Bela Sarmento Ribeiro4, M Filomena Botelho2, Maria I L Soares5, Andreia S R Oliveira5, Teresa M V D Pinho e Melo6.   

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.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

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

Mesh:

Substances:

Year:  2014        PMID: 24747064     DOI: 10.1016/j.ejmech.2014.04.008

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  5 in total

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