Abstract
The stilbene scaffold is a basic element for a number of biologically active natural and synthetic compounds, and it is considered as a privileged structure. Stilbenes exemplified by resveratrol, combretastatin A-4 and pterostilbene are of significant interest for drug research and development because of their potential in therapeutic and preventive application. Resveratrol, present in grapes and other food products, plays a role in the prevention of several human pathological processes and has been suggested as an anticancer agent. Moreover, recent evidence has revealed its potential effect on the aging process, diabetes and neurological dysfunction. Combretastatin A-4, from the bark of South African bush willow Combretum caffrum, also shows significant antitumor activity. Pterostilbene is closely related to resveratrol, sharing the same unique therapeutic potential as anti-inflammatory, antineoplastic and antioxidant agent.
Therefore, research and development of stilbene-based medicinal chemistry have become rapidly evolving and increasingly active topics covering almost the whole range of therapeutic fields.
In the present review, we provide an overview of the role of stilbenes in medicinal chemistry. In this context, we highlight the chemical methodologies adopted for the synthesis of stilbene derivatives, and outline the successful design of novel stilbene based hybrids in the field of cancer, Alzheimer’s and other relevant diseases. This information may be useful in further design of stilbene-based molecules as new leads for the development of novel agents with clinical potential or as effective chemical probes to dissect biological processes.
Keywords: Alkene arylation, Alzheimer’s disease, Cancer, Combretastatin, Diethylstilbestrol, Double bond formation, Hybrid compounds, Resveratrol.
Current Medicinal Chemistry
Title:The Use of Stilbene Scaffold in Medicinal Chemistry and Multi- Target Drug Design
Volume: 23 Issue: 23
Author(s): Elisa Giacomini, Sebastiano Rupiani, Laura Guidotti, Maurizio Recanatini and Marinella Roberti
Affiliation:
Keywords: Alkene arylation, Alzheimer’s disease, Cancer, Combretastatin, Diethylstilbestrol, Double bond formation, Hybrid compounds, Resveratrol.
Abstract: The stilbene scaffold is a basic element for a number of biologically active natural and synthetic compounds, and it is considered as a privileged structure. Stilbenes exemplified by resveratrol, combretastatin A-4 and pterostilbene are of significant interest for drug research and development because of their potential in therapeutic and preventive application. Resveratrol, present in grapes and other food products, plays a role in the prevention of several human pathological processes and has been suggested as an anticancer agent. Moreover, recent evidence has revealed its potential effect on the aging process, diabetes and neurological dysfunction. Combretastatin A-4, from the bark of South African bush willow Combretum caffrum, also shows significant antitumor activity. Pterostilbene is closely related to resveratrol, sharing the same unique therapeutic potential as anti-inflammatory, antineoplastic and antioxidant agent.
Therefore, research and development of stilbene-based medicinal chemistry have become rapidly evolving and increasingly active topics covering almost the whole range of therapeutic fields.
In the present review, we provide an overview of the role of stilbenes in medicinal chemistry. In this context, we highlight the chemical methodologies adopted for the synthesis of stilbene derivatives, and outline the successful design of novel stilbene based hybrids in the field of cancer, Alzheimer’s and other relevant diseases. This information may be useful in further design of stilbene-based molecules as new leads for the development of novel agents with clinical potential or as effective chemical probes to dissect biological processes.
Export Options
About this article
Cite this article as:
Giacomini Elisa, Rupiani Sebastiano, Guidotti Laura, Recanatini Maurizio and Roberti Marinella, The Use of Stilbene Scaffold in Medicinal Chemistry and Multi- Target Drug Design, Current Medicinal Chemistry 2016; 23 (23) . https://dx.doi.org/10.2174/0929867323666160517121629
DOI https://dx.doi.org/10.2174/0929867323666160517121629 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- 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
- Announcements
Related Articles
-
New Approaches in the Management of Septic Shock
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Cellular Membrane Microparticles: Potential Targets of Combinational Therapy for Vascular Disease
Current Vascular Pharmacology Protease Inhibitors in the Clinic
Medicinal Chemistry Structure and Function of the Human Breast Cancer Resistance Protein (BCRP/ABCG2)
Current Drug Metabolism Synthesis and In-Vitro Antitumor Activity of Selected 7-Fluoro-6-(4-methyl-1-piperazinyl)-2-(thiosubstituted)-4(3H)-quinazolinones
Letters in Organic Chemistry Peptide-based Self-assembly: Design, Bioactive Properties, and Its Applications
Current Pharmaceutical Design “Ayurvedic System”: A New Possible Safe and Effective way to get Rid of this Critical COVID-19 Pandemic Situation- A Review
Current Traditional Medicine Laboratory Techniques for Human Viral Encephalitis Diagnosis
Infectious Disorders - Drug Targets Novel Concepts for Anti-Infective Activity of Cytokines, Chemokines and Diverse Agents
Recent Patents on Anti-Infective Drug Discovery Synthesis, Molecular Docking, c-Met Inhibitions of 2,2,2-Trichloroethylidene- cyclohexane-1, 3-dione Derivatives Together with their Application as Target SARS-CoV-2 main Protease (Mpro) and as Potential anti-COVID-19
Combinatorial Chemistry & High Throughput Screening Multi-Targeted Molecular Docking and Drug-Likeness Evaluation of some Nitrogen Heterocyclic Compounds Targeting Proteins Involved in the Development of COVID-19
Medicinal Chemistry Cluster Analysis of Coronavirus Sequences using Computational Sequence Descriptors: With Applications to SARS, MERS and SARS-CoV-2 (CoVID-19)
Current Computer-Aided Drug Design The Metabolism of Anticancer Drugs by the Liver: Current Approaches to the Drug Development Process
Current Drug Metabolism Two-Dimensional (2D) In Silico Models for Absorption, Distribution, Metabolism, Excretion and Toxicity (ADME/T) in Drug Discovery
Current Topics in Medicinal Chemistry Induction of a Robust Humoral Response using HIV-1 VLP<sup>MPER-V3</sup> as a Novel Candidate Vaccine in BALB/c Mice
Current HIV Research Permeability for Intestinal Absorption: Caco-2 Assay and Related Issues
Current Drug Metabolism Computer-Aided Drug Design: Lead Discovery and Optimization
Combinatorial Chemistry & High Throughput Screening Decision Tree Methods in Pharmaceutical Research
Current Topics in Medicinal Chemistry Pharmacological Management of Acutely Agitated Schizophrenic Patients
Current Pharmaceutical Design Congenital Anomalies of the Urinary Tract
Current Pediatric Reviews