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.
Letters in Drug Design & Discovery
Title:4-Substituted-2-Methoxyphenol: Suitable Building Block to Prepare New Bioactive Natural-like Hydroxylated Biphenyls
Volume: 12 Issue: 2
Author(s): Maria Antonietta Dettori, Davide Fabbri, Marina Pisano, Carla Rozzo, Giuseppe Palmieri, Alessandro Dessi, Roberto Dallocchio and Giovanna Delogu
Affiliation:
Keywords: Curcumin, dihedral angle, hydroxylated biphenyls, malignant melanoma, synthesis.
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.
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Dettori Antonietta Maria, Fabbri Davide, Pisano Marina, Rozzo Carla, Palmieri Giuseppe, Dessi Alessandro, Dallocchio Roberto and Delogu Giovanna, 4-Substituted-2-Methoxyphenol: Suitable Building Block to Prepare New Bioactive Natural-like Hydroxylated Biphenyls, Letters in Drug Design & Discovery 2015; 12 (2) . https://dx.doi.org/10.2174/1570180811666140915222343
DOI https://dx.doi.org/10.2174/1570180811666140915222343 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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