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).
Synthesis and antitumor activity of α-alkyliden-γ-lactones
FRANCESCA CATENI;PATRIZIA NITTI;MARINA ZACCHIGNA;GIUSEPPE PROCIDA;LUCIA LASSIANI;SARA DRIOLI;CHIARA FLORIO;MARCO PELIN
2018-01-01
Abstract
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).File | Dimensione | Formato | |
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