Abstract
There is an emerging paradigm shift in oncology that seeks to emphasize molecularly targeted approaches for cancer prevention and therapy. Chalcones (1,3-diphenyl-2-propen-1-ones), naturally-occurring compounds with widespread distribution in spices, tea, beer, fruits and vegetables, consist of open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α, β-unsaturated carbonyl system. Due to their structural diversity, relative ease of chemical manipulation and reaction of α, β-unsaturated carbonyl moiety with cysteine residues in proteins, some lead chalcones from both natural products and synthesis have been identified in a variety of screening assays for modulating important pathways or molecular targets in cancers. These pathways and targets that are affected by chalcones include MDM2/p53, tubulin, proteasome, NF-kappa B, TRIAL/death receptors and mitochondria mediated apoptotic pathways, cell cycle, STAT3, AP-1, NRF2, AR, ER, PPAR-γ and β-catenin/Wnt. Compared to current cancer targeted therapeutic drugs, chalcones have the advantages of being inexpensive, easily available and less toxic; the ease of synthesis of chalcones from substituted benzaldehydes and acetophenones also makes them an attractive drug scaffold. Therefore, this review is focused on molecular targets of chalcones and their potential implications in cancer prevention and therapy.
Keywords: Chalcones, molecular targets, bioactive dietary compounds, chemoprevention.
Current Cancer Drug Targets
Title:Molecular Targeted Approaches to Cancer Therapy and Prevention Using Chalcones
Volume: 14 Issue: 2
Author(s): Danielle D. Jandial, Christopher A. Blair, Saiyang Zhang, Lauren S. Krill, Yan-Bing Zhang and Xiaolin Zi
Affiliation:
Keywords: Chalcones, molecular targets, bioactive dietary compounds, chemoprevention.
Abstract: There is an emerging paradigm shift in oncology that seeks to emphasize molecularly targeted approaches for cancer prevention and therapy. Chalcones (1,3-diphenyl-2-propen-1-ones), naturally-occurring compounds with widespread distribution in spices, tea, beer, fruits and vegetables, consist of open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α, β-unsaturated carbonyl system. Due to their structural diversity, relative ease of chemical manipulation and reaction of α, β-unsaturated carbonyl moiety with cysteine residues in proteins, some lead chalcones from both natural products and synthesis have been identified in a variety of screening assays for modulating important pathways or molecular targets in cancers. These pathways and targets that are affected by chalcones include MDM2/p53, tubulin, proteasome, NF-kappa B, TRIAL/death receptors and mitochondria mediated apoptotic pathways, cell cycle, STAT3, AP-1, NRF2, AR, ER, PPAR-γ and β-catenin/Wnt. Compared to current cancer targeted therapeutic drugs, chalcones have the advantages of being inexpensive, easily available and less toxic; the ease of synthesis of chalcones from substituted benzaldehydes and acetophenones also makes them an attractive drug scaffold. Therefore, this review is focused on molecular targets of chalcones and their potential implications in cancer prevention and therapy.
Export Options
About this article
Cite this article as:
Jandial D. Danielle, Blair A. Christopher, Zhang Saiyang, Krill S. Lauren, Zhang Yan-Bing and Zi Xiaolin, Molecular Targeted Approaches to Cancer Therapy and Prevention Using Chalcones, Current Cancer Drug Targets 2014; 14 (2) . https://dx.doi.org/10.2174/1568009614666140122160515
DOI https://dx.doi.org/10.2174/1568009614666140122160515 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...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
Related Articles
-
Pharmacotherapy in Systemic Lupus Erythematosus
Current Rheumatology Reviews Thymidine Phosphorylase and Fluoropyrimidines Efficacy: A Jekyl and Hyde Story
Current Medicinal Chemistry - Anti-Cancer Agents Fabrication of Multi-functionalized Gold Nanoparticles and the Application to Electrochemical Detection of Nitrite
Current Nanoscience Emerging Roles for Modulation of microRNA Signatures in Cancer Chemoprevention
Current Cancer Drug Targets Construction and Validation of a Nomogram for Predicting Progression- Free Survival in Patients with Early-Stage Testicular Germ Cell Tumor
Recent Patents on Anti-Cancer Drug Discovery Review of PI3K/mTOR Inhibitors Entering Clinical Trials to Treat Triple Negative Breast Cancers
Recent Patents on Anti-Cancer Drug Discovery Design of New Improved Curcumin Derivatives to Multi-targets of Cancer and Inflammation
Current Drug Targets Serum miRNAs Signature Plays an Important Role in Keloid Disease
Current Molecular Medicine Glyoxalase 1 and 2 Enzyme Inhibitory Activity of 6-Sulfamoylsaccharin and Sulfocoumarin Derivates
Letters in Drug Design & Discovery Lipoxygenase Inhibitors for Cancer Prevention: Promises and Risks
Current Pharmaceutical Design Meet Our Editorial Board Member:
Current Medicinal Chemistry Heterocyclic Scaffolds: Centrality in Anticancer Drug Development
Current Drug Targets Editorial (Thematic Issue: “miRNA and Cancer; Computational and Experimental Approaches”)
Current Pharmaceutical Biotechnology Anti-Inflammatory Drugs and Prediction of New Structures by Comparative Analysis
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Artificial Virus as Trump-card to Resolve Exigencies in Targeted Gene Delivery
Mini-Reviews in Medicinal Chemistry Overcoming Resistance of Glioblastoma to Conventional Cytotoxic Therapies by the Addition of PARP Inhibitors
Anti-Cancer Agents in Medicinal Chemistry Breaking the DNA Damage Response via Serine/Threonine Kinase Inhibitors to Improve Cancer Treatment
Current Medicinal Chemistry Drugs Made of RNA: Development and Application of Engineered RNAs for Gene Therapy
Mini-Reviews in Medicinal Chemistry Antisense Targets to Enhance Hormone and Cytotoxic Therapies in Advanced Prostate Cancer
Current Drug Targets Synthesis, Radiosynthesis and Metabolism of 131I-Y-c(CGRRAGGSC)
Anti-Cancer Agents in Medicinal Chemistry