Abstract
Curcumin, a natural diaryl heptanoid continues to be used as an alternative medicinal agent in many parts of South East Asia for treatment of many ailments. It can be usually obtained from substituted aryl aldehydes and acetylacetone and this route enables synthesis of a diverse set of curcumin analogues. Numerous analogues have been synthesized and tested by several researchers to investigate their activity against known biological targets and to improve upon the pharmacological and ADME profile by modifying substitutions on aromatic rings, β-diketone moiety and two flanking double bonds conjugated to the β-diketone moiety. Successful synthesis of such derivatives with modifications has resulted in the development of potential anticancer candidates that target various stages in cancer cell growth and development. Based on the evidences in modifications of these three functional elements, we have attempted to summarize the structure activity relationship of molecules which can be further utilized by researchers in medicinal chemistry in exploring the structure of curcumin.
Keywords: Curcumin, Anticancer activity of curcumin, SAR, potent derivatives of curcumin.
Mini-Reviews in Medicinal Chemistry
Title:A Comprehensive Review on SAR of Curcumin
Volume: 13 Issue: 12
Author(s): A. Rajasekhar Reddy, P. Dinesh, A.S. Prabhakar, K. Umasankar, B. Shireesha and M. Bhagavan Raju
Affiliation:
Keywords: Curcumin, Anticancer activity of curcumin, SAR, potent derivatives of curcumin.
Abstract: Curcumin, a natural diaryl heptanoid continues to be used as an alternative medicinal agent in many parts of South East Asia for treatment of many ailments. It can be usually obtained from substituted aryl aldehydes and acetylacetone and this route enables synthesis of a diverse set of curcumin analogues. Numerous analogues have been synthesized and tested by several researchers to investigate their activity against known biological targets and to improve upon the pharmacological and ADME profile by modifying substitutions on aromatic rings, β-diketone moiety and two flanking double bonds conjugated to the β-diketone moiety. Successful synthesis of such derivatives with modifications has resulted in the development of potential anticancer candidates that target various stages in cancer cell growth and development. Based on the evidences in modifications of these three functional elements, we have attempted to summarize the structure activity relationship of molecules which can be further utilized by researchers in medicinal chemistry in exploring the structure of curcumin.
Export Options
About this article
Cite this article as:
Reddy Rajasekhar A., Dinesh P., Prabhakar A.S., Umasankar K., Shireesha B. and Raju Bhagavan M., A Comprehensive Review on SAR of Curcumin, Mini-Reviews in Medicinal Chemistry 2013; 13 (12) . https://dx.doi.org/10.2174/1389557511313120007
DOI https://dx.doi.org/10.2174/1389557511313120007 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
Scintigraphic Imaging of Inflammatory Processes
Medicinal Chemistry Reviews - Online (Discontinued) Development of Genomics-Based Gene Expression Signature Biomarkers in Oncology and Toxicology to Facilitate Drug Discovery and Translational Medicine
Current Bioinformatics The Pathophysiological Role of PEDF in Bone Diseases
Current Molecular Medicine The Blood-Brain Barrier in Multiple Sclerosis: microRNAs as Key Regulators
CNS & Neurological Disorders - Drug Targets The Cross-talk between Tristetraprolin and Cytokines in Cancer
Anti-Cancer Agents in Medicinal Chemistry Identifying Biomarkers of Lung Cancer in the Post-Genomic Era
Current Pharmacogenomics Subject Index To Volume 1
Recent Patents on Anti-Cancer Drug Discovery Integrin αvβ3 as a Therapeutic Target for Blocking Tumor-Induced Angiogenesis
Current Drug Targets High Frequency of the Opioid Receptor µ-1 (OPRM1) A118G Polymorphism, an Opioid Drug Therapy Related Gene, in the Indonesian Population
Current Pharmacogenomics and Personalized Medicine Aptamers Overview: Selection, Features and Applications
Current Topics in Medicinal Chemistry The Use of Ghrelin and Ghrelin Receptor Agonists as a Treatment for Animal Models of Disease: Efficacy and Mechanism
Current Pharmaceutical Design A Multiwave Imaging Approach for Elastography
Current Medical Imaging Dietary Quercetin Alleviated DSS-induced Colitis in Mice Through Several Possible Pathways by Transcriptome Analysis
Current Pharmaceutical Biotechnology Acoustic Radiation Force Impulse (ARFI) Imaging: A Review
Current Medical Imaging The Yin and Yang of CD4+ Regulatory T Cells in Autoimmunity and Cancer
Current Medicinal Chemistry Barminomycin, a Model for the Development of New Anthracyclines
Anti-Cancer Agents in Medicinal Chemistry Therapeutic Applications of Crocus sativus L. (Saffron): A Review
The Natural Products Journal The Dark Side of Stem Cells: Triggering Cancer Progression by Cell Fusion
Current Molecular Medicine Poly (D, L-Lactide) Nanosuspensions of Risperidone for Parenteral Delivery: Formulation and In-Vitro Evaluation
Current Drug Delivery HPV Pathway Profiling: HPV Related Cervical Dysplasia and Carcinoma Studies
Current Pharmaceutical Design