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

Author(s): Maria Antonietta Dettori, Davide Fabbri, Marina Pisano, Carla Rozzo, Giuseppe Palmieri, Alessandro Dessi, Roberto Dallocchio, Giovanna Delogu.

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 2 , 2015

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Graphical 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.

Keywords: Curcumin, dihedral angle, hydroxylated biphenyls, malignant melanoma, synthesis.

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Article Details

Year: 2015
Page: [131 - 139]
Pages: 9
DOI: 10.2174/1570180811666140915222343

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PDF: 67