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

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.

SUBMITTER: Dettori MA

PROVIDER: S-EPMC4462845 | biostudies-literature | 2015 Feb

REPOSITORIES: biostudies-literature

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

Dettori Maria Antonietta MA Fabbri Davide D Pisano Marina M Rozzo Carla C Palmieri Giuseppe G Dess Alessandro A Dallocchio Roberto R Delogu Giovanna G

Letters in drug design & discovery 20150201 2

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 <i>in vitro</i>. Two curcumin-biphenyl derivatives showed interesting growth inhibitory activities on different malignant melanoma cell lines with IC<sub>50</sub> ranging from 13 to 1 µM. Preliminary molecular modeling studies were carried out to evaluate conformations and dihedral angle ...[more]

PMID: 26074750

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