Abstract
Chalcone or (E)-1,3-diphenyl-2-propene-1-one scaffold has gained considerable scientific interest in medicinal chemistry owing to its simple chemistry, ease in synthesizing a variety of derivatives and exhibiting a broad range of promising pharmacological activities by modulating several molecular targets. A number of natural and (semi-) synthetic chalcone derivatives have demonstrated admirable anti-inflammatory activity due to their inhibitory potential against various therapeutic targets like Cyclooxygenase (COX), Lipooxygenase (LOX), Interleukins (IL), Prostaglandins (PGs), Nitric Oxide Synthase (NOS), Leukotriene D4 (LTD4), Nuclear Factor-κB (NF- κB), Intracellular Cell Adhesion Molecule-1 (ICAM-1), Vascular Cell Adhesion Molecule-1 (VCAM-1), Monocyte Chemoattractant Protein-1 (MCP-1) and TLR4/MD-2, etc. The chalcone scaffold with hydroxyl, methoxyl, carboxyl, prenyl group and/or heterocyclic ring substitution like thiophene/furan/indole showed promising anti-inflammatory activity. In this review, a comprehensive study (from the year 1991 to 2016) on multi-targets of inflammatory interest, related inflammation reactions and their treatment by chalcone-based inhibitors acting on various molecular targets entailed in inflammation, Structure-Activity Relationships (SARs), Mechanism of Actions (MOAs), and patents are highlighted.
Keywords: Chalcone, inflammatory, inhibitor, patent, pathway, target.
Current Topics in Medicinal Chemistry
Title:Chalcone Derivatives: Anti-inflammatory Potential and Molecular Targets Perspectives
Volume: 17 Issue: 28
Author(s): Debarshi Kar Mahapatra, Sanjay Kumar Bharti*Vivek Asati
Affiliation:
- Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur - 495009, Chhattisgarh,India
Keywords: Chalcone, inflammatory, inhibitor, patent, pathway, target.
Abstract: Chalcone or (E)-1,3-diphenyl-2-propene-1-one scaffold has gained considerable scientific interest in medicinal chemistry owing to its simple chemistry, ease in synthesizing a variety of derivatives and exhibiting a broad range of promising pharmacological activities by modulating several molecular targets. A number of natural and (semi-) synthetic chalcone derivatives have demonstrated admirable anti-inflammatory activity due to their inhibitory potential against various therapeutic targets like Cyclooxygenase (COX), Lipooxygenase (LOX), Interleukins (IL), Prostaglandins (PGs), Nitric Oxide Synthase (NOS), Leukotriene D4 (LTD4), Nuclear Factor-κB (NF- κB), Intracellular Cell Adhesion Molecule-1 (ICAM-1), Vascular Cell Adhesion Molecule-1 (VCAM-1), Monocyte Chemoattractant Protein-1 (MCP-1) and TLR4/MD-2, etc. The chalcone scaffold with hydroxyl, methoxyl, carboxyl, prenyl group and/or heterocyclic ring substitution like thiophene/furan/indole showed promising anti-inflammatory activity. In this review, a comprehensive study (from the year 1991 to 2016) on multi-targets of inflammatory interest, related inflammation reactions and their treatment by chalcone-based inhibitors acting on various molecular targets entailed in inflammation, Structure-Activity Relationships (SARs), Mechanism of Actions (MOAs), and patents are highlighted.
Export Options
About this article
Cite this article as:
Mahapatra Kar Debarshi , Bharti Kumar Sanjay *, Asati Vivek , Chalcone Derivatives: Anti-inflammatory Potential and Molecular Targets Perspectives, Current Topics in Medicinal Chemistry 2017; 17 (28) . https://dx.doi.org/10.2174/1568026617666170914160446
DOI https://dx.doi.org/10.2174/1568026617666170914160446 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Adaptogens—History and Future Perspectives
Adaptogens are pharmacologically active compounds or plant extracts that are associated with the ability to enhance the body’s stability against stress. The intake of adaptogens is associated not only with a better ability to adapt to stress and maintain or normalise metabolic functions but also with better mental and physical ...read more
Addressing the Most Common Causes of Death with Niacin/NAD and Inositol Polyphosphates
The most common causes of death in the world are cardiovascular disease (CVD) and cancer. These are perhaps best addressed by reducing lipodystrophy and blockages with niacin and inositol polyphosphates (e.g., IP6+inositol) respectively when addressing CVD. Niacin serves as a vitamin by virtue of its role as a skeletal precursor ...read more
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more

- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
Protein Oxidative Modification in the Aging Organism and the Role of the Ubiquitin Proteasomal System
Current Pharmaceutical Design Bioplex Technology: Novel Synthetic Gene Delivery Pharmaceutical Based on Peptides Anchored to Nucleic Acids
Current Pharmaceutical Design Deletion of Endoplasmic Reticulum Stress-Induced CHOP Protects Microvasculature Post-Spinal Cord Injury
Current Neurovascular Research Medicinal Agents in the Metabolic Syndrome
Cardiovascular & Hematological Agents in Medicinal Chemistry PET Imaging of the Peripheral Benzodiazepine Receptor: Monitoring Disease Progression and Therapy Response in Neurodegenerative Disorders
Current Pharmaceutical Design From the Stretcher to the Pharmacys Shelf: Drug Leads from Medically Important Brazilian Venomous Arachnid Species
Inflammation & Allergy - Drug Targets (Discontinued) Heterocyclic Naphthalimides as New Skeleton Structure of Compounds with Increasingly Expanding Relational Medicinal Applications
Current Topics in Medicinal Chemistry Recent Advances in Oncogenic Roles of the TRPM7 Chanzyme
Current Medicinal Chemistry Pyrazolopyrimidine Derivatives as Antineoplastic Agents: with a Special Focus on Thyroid Cancer
Mini-Reviews in Medicinal Chemistry Benzoin Schiff Bases: Design, Synthesis, and Biological Evaluation as Potential Antitumor Agents
Medicinal Chemistry A Concise Review on the Role of Natural and Synthetically Derived Peptides in Colorectal Cancer
Current Topics in Medicinal Chemistry Advances in the Design and Development of PROTAC-mediated HDAC Degradation
Current Topics in Medicinal Chemistry Vasoactive Intestinal Peptide in Neurodevelopmental Disorders:Therapeutic Potential
Current Pharmaceutical Design Development and Applications of Non-HIV-Based Lentiviral Vectors in Neurological Disorders
Current Gene Therapy Cytoprotective Effect of Phenolic Extract from Brazilian Apple Peel in Insulin-Producing Cells
Current Nutrition & Food Science New Approaches for the Treatment of Allergic Conditions
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents A Comprehensive Overview of Colon Cancer- A Grim Reaper of the 21st Century
Current Medicinal Chemistry Immune Mechanisms and Novel Pharmacological Therapies of Acute Kidney Injury
Current Drug Targets Activated Protein C and Acute Kidney Injury: Selective Targeting of PAR-1
Current Drug Targets The Potential Role of Pro-Inflammatory and Anti-Inflammatory Cytokines in Epilepsy Pathogenesis
Endocrine, Metabolic & Immune Disorders - Drug Targets