New synthetic inhibitors of fatty acid synthase with anticancer activity

…, M Artola, B Benhamú, S Ortega-Gutiérrez…

Index: Turrado, Carlos; Puig, Teresa; Garcia-Carceles, Javier; Artola, Marta; Benhamu, Bellinda; Ortega-Gutierrez, Silvia; Relat, Joana; Oliveras, Gloria; Blancafort, Adriana; Haro, Diego; Marrero, Pedro F.; Colomer, Ramon; Lopez-Rodriguez, Maria L. Journal of Medicinal Chemistry, 2012 , vol. 55, # 11 p. 5013 - 5023

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Citation Number: 31

Abstract

Fatty 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 μM have been tested for their ability to inhibit FASN activity. Among them, derivative 30 blocks the 90% of FASN ...