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.
Export Options
About this article
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
DOI https://dx.doi.org/10.2174/1570180811666140915222343 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Editorial
Recent Patents on Anti-Cancer Drug Discovery The PI3K Pathway at the Crossroads of Cancer and the Immune System: Strategies for Next Generation Immunotherapy Combinations
Current Cancer Drug Targets Boron Nitride Nanotubes: Production, Properties, Biological Interactions and Potential Applications as Therapeutic Agents in Brain Diseases
Current Nanoscience Effects of Lipid Composition and Preparation Conditions on Physical-Chemical Properties, Technological Parameters and In Vitro Biological Activity of Gemcitabine-Loaded Liposomes
Current Drug Delivery Plasminogen Activator System and Vascular Disease
Current Vascular Pharmacology Overview of Naphthalimide Analogs as Anticancer Agents
Current Medicinal Chemistry Functional and Molecular Ultrasound Imaging: Concepts and Contrast Agents
Current Medicinal Chemistry Frequency of Depression and its Correlation with Serum Carnitine Level in HIV/AIDS Patients
Current HIV Research Quinone Methides as DNA Alkylating Agents: An Overview on Efficient Activation Protocols for Enhanced Target Selectivity
Current Organic Chemistry Nanoparticle-Delivered Quercetin for Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Retinoic Acid Signaling in P19 Stem Cell Differentiation
Anti-Cancer Agents in Medicinal Chemistry Cellular Protection and Therapeutic Potential of Tocotrienols
Current Pharmaceutical Design Immune Checkpoint Inhibitor Therapy and Risk of Myocarditis: A Review of the Literature
Current Immunology Reviews (Discontinued) Optimization on Fc for Improvement of Stability and Aggregation Resistance
Current Pharmaceutical Biotechnology Hypertension, Anti-Hypertensive Therapy and Neoplasia
Current Pharmaceutical Design IT-143, A Polymer Micelle Nanoparticle, Widens Therapeutic Window of Daunorubicin
Pharmaceutical Nanotechnology Glucose-6-phosphate Dehydrogenase: a Biomarker and Potential Therapeutic Target for Cancer
Anti-Cancer Agents in Medicinal Chemistry Perspectives on Sesquiterpene Lactones in Inflammation and Cancer
Current Drug Targets Meet Our Editorial Board Member
Current Medicinal Chemistry Hydrophilic Interaction Liquid Chromatography Tandem Mass Spectrometry: An Attractive and Prospective Method for Quantitative Bioanalysis in Drug Metabolism
Current Drug Metabolism