European Journal of Medicinal Chemistry (2020)
Update date:2022-08-03
Topics:
Dupommier, Dorian
Muller, Claire
Comoy, Corinne
Mazerbourg, Sabine
Bordessa, Andrea
Piquard, Eline
Pawlak, Manon
Piquard, Flavian
Martin, Hélène
De Fays, Elia
Grandemange, Stéphanie
Flament, Stéphane
Boisbrun, Michel
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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