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.
View MoreKunming Biohome Technology Co. Ltd.
website:http://www.biohometech.com/
Contact:86-871-67428869
Address:kunming
shanghai jiuling chemical co.,ltd.
Contact:+86-21-50387295
Address:Zaozhuang Road, Pudong, Shanghai City. China
Huludao Tianqi Shengye Chemical Co.,Ltd.
Contact:0086 429 2075777
Address:Area B,Shipbuilding Industry Park,Beigang District,Huludao City,Liaoning prov.,China
Contact:86-25-58619180
Address:Nanjing High-Tech Zone 10 Xinghuo Road Pukou District Nanjing, Jiangsu 210061 The People's Republic of China
Contact:+1-416-493-6870
Address:Toronto, Canada
Doi:10.1016/S0040-4020(01)86594-7
(1992)Doi:10.1021/jo401398n
(2013)Doi:10.1002/recl.19921111002
(1992)Doi:10.1021/jo4011409
(2013)Doi:10.1002/anie.201502975
(2015)Doi:10.1002/ejoc.201200985
(2012)