Synthesis and antitumor activity of α-alkyliden-γ-lactones

Citation data:

International Journal of Pharmaceutical Research, ISSN: 0975-2366, Vol: 10, Issue: 4, Page: 1-8

Publication Year:
2018

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DOI:
10.31838/ijpr/2018.10.04.001
Author(s):
Francesca Cateni; Patrizia Nitti; Marina Zacchigna; Giuseppe Procida; Lucia Lassiani; Sara Drioli; Chiara Florio; Marco Pelin
Publisher(s):
SynthesisHub Advance Scientific Research
Tags:
Pharmacology, Toxicology and Pharmaceutics
article description
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-γ 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).