New desulfured troglitazone derivatives: Improved synthesis and biological evaluation
| Autor: | Flavian Piquard, Claire Muller, Manon Pawlak, Eline Piquard, Elia de Fays, Michel Boisbrun, Hélène Martin, Stéphanie Grandemange, Stéphane Flament, Dorian Dupommier, Corinne Comoy, Sabine Mazerbourg, Andrea Bordessa |
|---|---|
| Přispěvatelé: | Laboratoire Lorrain de Chimie Moléculaire (L2CM), Institut de Chimie du CNRS (INC)-Université de Lorraine (UL)-Centre National de la Recherche Scientifique (CNRS), Centre de Recherche en Automatique de Nancy (CRAN), Centre National de la Recherche Scientifique (CNRS)-Université de Lorraine (UL), Fonctions et dysfonctions épithéliales - UFC (EA 4267) (FDE), Université de Franche-Comté (UFC), Université Bourgogne Franche-Comté [COMUE] (UBFC)-Université Bourgogne Franche-Comté [COMUE] (UBFC) |
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Cell cycle checkpoint
Context (language use) Antineoplastic Agents Apoptosis [CHIM.THER]Chemical Sciences/Medicinal Chemistry 01 natural sciences 03 medical and health sciences chemistry.chemical_compound Structure-Activity Relationship Troglitazone Breast cancer Drug Discovery medicine Humans Cells Cultured 030304 developmental biology Cell Proliferation Pharmacology 0303 health sciences Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry [CHIM.ORGA]Chemical Sciences/Organic chemistry Organic Chemistry Chromane General Medicine Cell Cycle Checkpoints Lipase medicine.disease In vitro 0104 chemical sciences 3. Good health Deracemization Cancer research Drug Screening Assays Antitumor Lead compound medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry European Journal of Medicinal Chemistry, Elsevier, 2020, 187, pp.111939. ⟨10.1016/j.ejmech.2019.111939⟩ |
| ISSN: | 0223-5234 1768-3254 |
| Popis: | International audience; 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. |
| Databáze: | OpenAIRE |
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