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:CNR-Istituto di Chimica Biomolecolare, UOS Sassari, Traversa La Crucca 3, 07100 Sassari-Baldinca Italy.
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.
