The α-methylene-γ-butyrolactone skeleton is part of many natural products with remarkable biological properties.
C75, a fatty acid synthase (FAS) inhibitor, is a synthetic α-methylene-γ-butyrolactone which is cytotoxic for different
cell lines in vitro and in vivo against human cancer xenografts. We synthesized a panel of C75 derivatives through
modifications of the α-methylene moiety at the C-β/C- carbons of the γ-butyrolactone skeleton and tested their
effects on different cancer models. The in vitro effects of the compounds on pancreatic, colon and breast cancer cell
viability (PANC-1, HTC-116, Lovo, MCF-7, MDA-231-MB) were evaluated. Two compounds showed significant
cytotoxicity. The structures of all synthesized compounds obtained were identified on the basis of their spectral data
(IR, MS, NMR).
