Abstract
Cancer and malaria are two major diseases, which have devastating effects on public health systems. In a quest of developing new anticancer and antimalarial agents, a series of 22 unsymmetrical C5-curcumionds was synthesized and evaluated for their anticancer activity against HeLa, KB, PC3 and DU145 cancer cell lines. Out of these, four compounds displayed potent activity in HeLa cancer cell line (IC50 ranging from 0.7 to 0.9 µM) than standard FDA-approved drug doxorubicin (IC50 = 1.7 µM). They also showed weak to moderate activity against other cancer cell lines. Unsymmetrical C5-curcumionids were also evaluated for their antimalarial activity against CQ-sensitive and CQ-resistant strains of P. falciparum. Weak antimalarial activities were observed with some compounds without any toxicity towards the mammalian cell line at the highest tested concentration of 10 µM.
Keywords: Anticancer activity, Antimalarial activity, Curcumin, C5-curcuminoids, HeLa cancer cell line, Plasmodium falciparum.
Letters in Drug Design & Discovery
Title:Synthesis of Unsymmetrical C5-Curcuminoids as Potential Anticancer Agents
Volume: 11 Issue: 2
Author(s): Sunny Manohar, Anuj Thakur, Shabana I. Khan, Guojing Sun, Nanting Ni, Binghe Wang and Diwan S. Rawat
Affiliation:
Keywords: Anticancer activity, Antimalarial activity, Curcumin, C5-curcuminoids, HeLa cancer cell line, Plasmodium falciparum.
Abstract: Cancer and malaria are two major diseases, which have devastating effects on public health systems. In a quest of developing new anticancer and antimalarial agents, a series of 22 unsymmetrical C5-curcumionds was synthesized and evaluated for their anticancer activity against HeLa, KB, PC3 and DU145 cancer cell lines. Out of these, four compounds displayed potent activity in HeLa cancer cell line (IC50 ranging from 0.7 to 0.9 µM) than standard FDA-approved drug doxorubicin (IC50 = 1.7 µM). They also showed weak to moderate activity against other cancer cell lines. Unsymmetrical C5-curcumionids were also evaluated for their antimalarial activity against CQ-sensitive and CQ-resistant strains of P. falciparum. Weak antimalarial activities were observed with some compounds without any toxicity towards the mammalian cell line at the highest tested concentration of 10 µM.
Export Options
About this article
Cite this article as:
Manohar Sunny, Thakur Anuj, I. Khan Shabana, Sun Guojing, Ni Nanting, Wang Binghe and S. Rawat Diwan, Synthesis of Unsymmetrical C5-Curcuminoids as Potential Anticancer Agents, Letters in Drug Design & Discovery 2014; 11 (2) . https://dx.doi.org/10.2174/15701808113109990061
DOI https://dx.doi.org/10.2174/15701808113109990061 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
How is Gene Transfection Able to Improve Current Chemotherapy? The Role of Combined Therapy in Cancer Treatment
Current Medicinal Chemistry The Sodium-Iodide Symporter
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Cigarette Smoking, Metabolic Activation and Carcinogenesis
Current Drug Metabolism Chemokine Network in the Nervous System: A New Target for Pain Relief
Current Medicinal Chemistry Potential Prophylactic and Therapeutic Vaccines for HSV Infections
Current Pharmaceutical Design Cellular Iron Homeostasis and Therapeutic Implications of Iron Chelators in Cancer
Current Pharmaceutical Biotechnology The Protein-Protein Interaction-Mediated Inactivation of PTEN
Current Molecular Medicine Alphavirus Vectors for Gene Therapy Applications
Current Gene Therapy Novel Concepts in the Development of Platinum Antitumor Drugs
Current Medicinal Chemistry - Anti-Cancer Agents Uncommon Becoming Common: Case Series of Primary Fallopian Tube Cancers
Current Women`s Health Reviews The GABAergic System and the Gastrointestinal Physiopathology
Current Pharmaceutical Design Therapeutic Application of Intrabodies Against Age-Related Neurodegenerative Disorders
Current Pharmaceutical Design Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents
Current Medicinal Chemistry Vitamin D Supplementation: A Promising Approach for the Prevention and Treatment of Strokes
Current Drug Targets Circular RNAs and Glioma: Small Molecule with Big Actions
Current Molecular Medicine 4-Anilinoquinazoline Derivatives with Epidermal Growth Factor Receptor Inhibitor Activity
Anti-Cancer Agents in Medicinal Chemistry A Systematic Review of Genes Involved in the Inverse Resistance Relationship Between Cisplatin and Paclitaxel Chemotherapy: Role of BRCA1
Current Cancer Drug Targets Anti-cancer Research on Arnebiae radix-derived Naphthoquinone in Recent Five Years
Recent Patents on Anti-Cancer Drug Discovery Synthesis, Characterization, Biological Evaluation and Molecular Docking Studies of New Oxoacrylate and Acetamide on HeLa Cancer Cell Lines
Current Computer-Aided Drug Design Poly(ADP-ribose) Polymerase-1 Inhibitor 3-Aminobenzamide Enhances Apoptosis Induction by Platinum Complexes in Cisplatin-Resistant Tumor Cells
Medicinal Chemistry