Turrado, CarlosPuig i Miquel, TeresaGarcía-Cárceles, JavierArtola Pino, MartaBenhamú, BellindaOrtega-Gutiérrez, SilviaRelat Pardo, JoanaOliveras Serrat, GlòriaBlancafort, AdrianaHaro Bautista, DiegoMarrero González, Pedro F.Colomer Bosch, RamónLópez-Rodríguez, María Luz2021-01-282021-01-282012-05-040022-2623https://hdl.handle.net/2445/173502Fatty acid synthase (FASN) is a lipogenic enzyme that is highly expressed in different human cancers. Here we report the development of a new series of polyphenolic compounds 5-­30 that have been evaluated for their cytotoxic capacity in SK-­Br3 cells, a human breast cancer cell line with high FASN expression. The compounds with an IC50 < 50 􀁐M have been tested for their ability to inhibit FASN activity. Among them, derivative 30 blocks the 90% of FASN activity at low concentration (4 􀁐M), is highly cytotoxic in a broad panel of tumor cells, induces apoptosis, and blocks the activation of HER2, AKT and ERK pathways. Remarkably, 30 does not activate carnitine palmitoyltransferase-­1 (CPT-­1) nor induces in mice weight loss, which are the main drawbacks of other previously described FASN inhibitors. Thus, FASN inhibitor 30 may aid the validation of this enzyme as a therapeutic target for the treatment of cancer.11 p.application/pdfeng(c) American Chemical Society , 2012Àcids grassosMetabolismeInhibidors enzimàticsFatty acidsMetabolismEnzyme inhibitorsinfo:eu-repo/semantics/article6138272021-01-28info:eu-repo/semantics/openAccess