New desulfured troglitazone derivatives: Improved synthesis and biological evaluation
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| Titre | New desulfured troglitazone derivatives: Improved synthesis and biological evaluation |
| Type de publication | Journal Article |
| Year of Publication | 2020 |
| Auteurs | Dupommier D, Muller C, Comoy C, Mazerbourg S, Bordessa A, Piquard E, Pawlak M, Piquard F, Martin H, De Fays E, Grandemange S, Flament S, Boisbrun M |
| Journal | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY |
| Volume | 187 |
| Pagination | 111939 |
| Date Published | FEB 1 |
| Type of Article | Article |
| ISSN | 0223-5234 |
| Mots-clés | Apoptosis, Breast cancer, Chromane, Deracemization, Lipase, Troglitazone |
| Résumé | 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. (C) 2019 Elsevier Masson SAS. All rights reserved. |
| DOI | 10.1016/j.ejmech.2019.111939 |