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

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.
AuthorsKathleen Santos, Mafalda Laranjo, Ana Margarida Abrantes, Ana F Brito, Cristina Gonçalves, Ana Bela Sarmento Ribeiro, M Filomena Botelho, Maria I L Soares, Andreia S R Oliveira, Teresa M V D Pinho e Melo
JournalEuropean journal of medicinal chemistry (Eur J Med Chem) Vol. 79 Pg. 273-81 (May 22 2014) ISSN: 1768-3254 [Electronic] France
PMID24747064 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2014 Elsevier Masson SAS. All rights reserved.
Chemical References
  • 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo(1,2-c)thiazole
  • Antineoplastic Agents
  • Pyrroles
  • Thiazoles
Topics
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Breast Neoplasms (drug therapy, metabolism, pathology)
  • Cell Cycle (drug effects)
  • Cell Death (drug effects)
  • Cell Proliferation (drug effects)
  • Cell Survival (drug effects)
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Female
  • Humans
  • MCF-7 Cells
  • Molecular Structure
  • Pyrroles (chemical synthesis, chemistry, pharmacology)
  • Structure-Activity Relationship
  • Thiazoles (chemical synthesis, chemistry, pharmacology)
  • Tumor Cells, Cultured

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