Abstract
A series of 4-piperidone based curcuminoids were synthesized and anticancer potential of these compounds was evaluated against human myeloid leukemia (KBM5) and colon cancer (HCT116) cell lines. Their anti-inflammatory potential was determined through the down-regulation of tumor necrosis factor (TNF)-α-induced nuclear factor (NF)-κB. All compounds, except one, were found to exhibit better cytotoxicity than curcumin at 5 μM. Furthermore, many compounds have shown good potential to inhibit the TNF-α-induced NF-κB activation. Docking study of the compounds with NF-κB revealed that the binding affinity of the compounds ranged from ‒9.0 to ‒6.5 kcal/mol with 0-8 H-bonds. It was also observed that amido-ether based mono-carbonyl compounds bound around the same region of NF-κB where polynucleotides are known to bind to exhibit their activity.
Keywords: Anti-inflammatory, anti-proliferation, chronic myeloid leukemia, curcumin, colon cancer, cytotoxicity.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis of 4-piperidone Based Curcuminoids with Anti-inflammatory and Anti-Proliferation Potential in Human Cancer Cell Lines
Volume: 16 Issue: 7
Author(s): Amit Anthwal, Kundan Singh, M. S.M. Rawat, Amit K. Tyagi, Ashanul Haque, Imran Ali and Diwan S. Rawat
Affiliation:
Keywords: Anti-inflammatory, anti-proliferation, chronic myeloid leukemia, curcumin, colon cancer, cytotoxicity.
Abstract: A series of 4-piperidone based curcuminoids were synthesized and anticancer potential of these compounds was evaluated against human myeloid leukemia (KBM5) and colon cancer (HCT116) cell lines. Their anti-inflammatory potential was determined through the down-regulation of tumor necrosis factor (TNF)-α-induced nuclear factor (NF)-κB. All compounds, except one, were found to exhibit better cytotoxicity than curcumin at 5 μM. Furthermore, many compounds have shown good potential to inhibit the TNF-α-induced NF-κB activation. Docking study of the compounds with NF-κB revealed that the binding affinity of the compounds ranged from ‒9.0 to ‒6.5 kcal/mol with 0-8 H-bonds. It was also observed that amido-ether based mono-carbonyl compounds bound around the same region of NF-κB where polynucleotides are known to bind to exhibit their activity.
Export Options
About this article
Cite this article as:
Anthwal Amit, Singh Kundan, S.M. Rawat M., K. Tyagi Amit, Haque Ashanul, Ali Imran and S. Rawat Diwan, Synthesis of 4-piperidone Based Curcuminoids with Anti-inflammatory and Anti-Proliferation Potential in Human Cancer Cell Lines, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (7) . https://dx.doi.org/10.2174/1871520616666160201151206
DOI https://dx.doi.org/10.2174/1871520616666160201151206 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Biomolecules as Host Defense Weapons Against Microbial Pathogens
Recent Patents on DNA & Gene Sequences Glioma Stem Cell Maintenance: The Role of the Microenvironment
Current Pharmaceutical Design Meridianins: Marine-Derived Potent Kinase Inhibitors
Mini-Reviews in Medicinal Chemistry SELDI Protein Chip Technology for the Detection of Serum Biomarkers for Liver Disease
Protein & Peptide Letters Self-Assembling Peptides: Potential Role in Tumor Targeting
Current Pharmaceutical Biotechnology Frequency of Pathological Types of Hyperthyroidism in Thyroid Scan Patients
Current Medical Imaging Isoliquiritigenin Inhibits Proliferation and Induces Apoptosis via Alleviating Hypoxia and Reducing Glycolysis in Mouse Melanoma B16F10 Cells
Recent Patents on Anti-Cancer Drug Discovery Pyridine Based Antitumour Compounds Acting at the Colchicine Site
Current Medicinal Chemistry Nonprofit Pharma: Solutions to What Ails the Industry
Current Medicinal Chemistry Phosphatidylinositol 3-Kinase Isoforms as Novel Drug Targets
Current Drug Targets Functional Chemical Groups that May Likely Become a Source for the Synthesis of Novel Central Nervous System (CNS) Acting Drugs
Central Nervous System Agents in Medicinal Chemistry In Vitro Regulatory Effect of Epididymal Serpin CRES on Protease Activity of Proprotein Convertase PC4/PCSK4
Current Molecular Medicine Mast Cells in Allergic and Inflammatory Diseases
Current Pharmaceutical Design Targeting Tumour Metastasis: The Emerging Role of Nanotechnology
Current Medicinal Chemistry Strain-Promoted Cycloadditions for Development of Copper-Free Click Reactions
Current Organic Chemistry Potential Therapeutic Benefits of Maintaining Mitochondrial Health in Peripheral Neuropathies
Current Neuropharmacology Polymeric Systems as Nanodevices for siRNA Delivery
Current Gene Therapy Is There a Clinical Future for Spermatogonial Stem Cells?
Current Stem Cell Research & Therapy Steroid Receptor-Associated Immunophilins: Candidates for Diverse Drug-Targeting Approaches in Disease
Current Molecular Pharmacology Role of Flavonoids in Future Anticancer Therapy by Eliminating the Cancer Stem Cells
Current Stem Cell Research & Therapy