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Synthesis and antitumor activity of a-alkyliden-?- lactones
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| Author:
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FRANCESCA CATENI*, PATRIZIA NITTI, MARINA ZACCHIGNA, GIUSEPPE PROCIDA, LUCIA LASSIANI, SARA DRIOLI, CHIARA FLORIO, MARCO PELIN
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| Abstract:
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The a-methylene-?-butyrolactone skeleton is part of many natural products with remarkable biological properties.
C75, a fatty acid synthase (FAS) inhibitor, is a synthetic a-methylene-?-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 a-methylene moiety at the C-ß/C-? carbons of the ?-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).
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| Keyword:
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a-methylene-?-butyrolactones; C75; cell viability; MTT assay
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| EOI:
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-
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| DOI:
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https://doi.org/10.31838/ijpr/2018.10.04.001
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| Download:
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