New desulfured troglitazone derivatives: Improved synthesis and biological evaluation.
Eur J Med Chem
; 187: 111939, 2020 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-31838327
ABSTRACT
Breast cancer is a major medical threat which cannot be sufficiently addressed by current therapies because of spontaneous or acquired treatment resistance. Besides, triple-negative breast cancer (TNBC) tumors do not respond to targeted therapies, thus new therapeutic strategies are needed. In this context, we designed and prepared new desulfured troglitazone (TGZ)-derived molecules and evaluated them in vitro for their anti-proliferative activity, with a special focus on triple-negative breast cancer cell lines. Optimization of the synthetic strategies and deracemization of the lead compound were performed to give highly active compound 10 with low-micromolar potency. Further studies revealed that this compound triggers apoptosis rather than cell cycle arrest as observed with TGZ.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Troglitazona
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article