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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

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Published by : Advanced Scientific Research
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0975-2366
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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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Synthesis and antitumor activity of a-alkyliden-?- lactones

Author: FRANCESCA CATENI*, PATRIZIA NITTI, MARINA ZACCHIGNA, GIUSEPPE PROCIDA, LUCIA LASSIANI, SARA DRIOLI, CHIARA FLORIO, MARCO PELIN
Abstract: 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).
Keyword: a-methylene-?-butyrolactones; C75; cell viability; MTT assay
DOI: https://doi.org/10.31838/ijpr/2018.10.04.001
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