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Bentham Science Publishers, Letters in Drug Design & Discovery, 2(12), p. 131-139

DOI: 10.2174/1570180811666140915222343

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4-Substituted-2-Methoxyphenol: Suitable Building Block to Prepare New Bioactive Natural-like Hydroxylated Biphenyls

Journal article published in 2014 by Maria Antonietta Dettori, Davide Fabbri, Marina Pisano ORCID, Carla Rozzo, Giuseppe Palmieri ORCID, Alessandro Dessµ, Alessandro Dessi, Alessandro Dessì, Roberto Dallocchio ORCID, Giovanna Delogu
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This paper is available in a repository.

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Abstract

A small collection of eugenol- and curcumin-analog hydroxylated biphenyls was prepared by straightforward methods starting from natural 4-substituted-2-methoxyphenols and their antitumoral activity was evaluated in vitro. Two curcumin-biphenyl derivatives showed interesting growth inhibitory activities on different malignant melanoma cell lines with IC50 ranging from 13 to 1 µM. Preliminary molecular modeling studies were carried out to evaluate conformations and dihedral angles suitable for antiproliferative activity in hydroxylated biphenyls bearing a side aliphatic chain.