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

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.

Cite this article as:

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