Abstract
In continuation of our study on anticancer compounds, a series of novel artemisinin dimers have been synthesized and evaluated for their cytotoxic effects against three human cancer cell lines, including HepG2 (liver cancer), MCF-7(breast cancer) and HL-60 (leukemia cancer). The assay results showed that most of the compounds displayed inhibitory effects against all three human cancer cell lines tested, and seemed to be more cytotoxic toward the blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells. Among the synthesized artemisinin dimers, the compound 10d with a double bond bridge exhibited the most potent cytotoxicity with IC50 values of 5.08, 4.82 and 1.32 µg/mL against the HepG2, MCF-7, and HL-60 cell lines, respectively.
Keywords: Artemisinin, cytotoxicity, antimalarial, cancer, dimer.
Letters in Drug Design & Discovery
Title:Novel Artemisinin-Derived Dimers: Synthesis and Evaluation of Anti-cancer Activities
Volume: 14 Issue: 1
Author(s): Vu Tuan Kien, Le Huy Binh, Phan Hai Phong, Doan Thi Hien, Nguyen Thi Thuy My, Nguyen Hai Nam, Do Thi Thao, Michael Baltas and Tran Khac Vua
Affiliation:
Keywords: Artemisinin, cytotoxicity, antimalarial, cancer, dimer.
Abstract: In continuation of our study on anticancer compounds, a series of novel artemisinin dimers have been synthesized and evaluated for their cytotoxic effects against three human cancer cell lines, including HepG2 (liver cancer), MCF-7(breast cancer) and HL-60 (leukemia cancer). The assay results showed that most of the compounds displayed inhibitory effects against all three human cancer cell lines tested, and seemed to be more cytotoxic toward the blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells. Among the synthesized artemisinin dimers, the compound 10d with a double bond bridge exhibited the most potent cytotoxicity with IC50 values of 5.08, 4.82 and 1.32 µg/mL against the HepG2, MCF-7, and HL-60 cell lines, respectively.
Export Options
About this article
Cite this article as:
Kien Tuan Vu, Binh Huy Le, Phong Hai Phan, Hien Thi Doan, My Thi Thuy Nguyen, Nam Hai Nguyen, Thao Thi Do, Baltas Michael and Vua Khac Tran, Novel Artemisinin-Derived Dimers: Synthesis and Evaluation of Anti-cancer Activities, Letters in Drug Design & Discovery 2017; 14(1) . https://dx.doi.org/10.2174/1570180813666160810155354
DOI https://dx.doi.org/10.2174/1570180813666160810155354 |
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
-
A Practical Perspective on the Evaluation of Small Molecule CNS Penetration in Drug Discovery
Drug Metabolism Letters Nutraceuticals for Protection and Healing of Gastrointestinal Mucosa
Current Medicinal Chemistry Cell-Penetrating Peptides as Delivery Enhancers for Vaccine
Current Pharmaceutical Biotechnology TNF-Related Apoptosis-Inducing Ligand (TRAIL) as a Pro-Apoptotic Signal Transducer with Cancer Therapeutic Potential
Current Pharmaceutical Design Recent Advances in the Development of Thioredoxin Reductase Inhibitors as Anticancer Agents
Current Drug Targets Immunomodulating and Anti-Allergic Effects of Negroamaro and Koshu Vitis vinifera Fermented Grape Marc (FGM)
Current Pharmaceutical Design Folate Deficiency and Aberrant Expression of DNA Methyltransferase 1 were Associated with Cervical Cancerization
Current Pharmaceutical Design Intelligent Polyelectrolytes and Gels in Oral Drug Delivery
Current Pharmaceutical Biotechnology Molecular Biotheranostic Approaches of Cancers Using LAT Kit Probes
Current Medical Imaging Implications of Nanotechnology in Healthcare
Nanoscience & Nanotechnology-Asia Telomere Length Variations in Aging and Age-Related Diseases
Current Aging Science Protein Tyrosine Signaling and its Potential Therapeutic Implications in Carcinogenesis
Current Pharmaceutical Design Targeting Hypoxia-Inducible Factor-1 (HIF-1) Signaling in Therapeutics: Implications for the Treatment of Inflammatory Bowel Disease
Recent Patents on Inflammation & Allergy Drug Discovery Enhanced Biocatalytic Activity of Recombinant Lipase Immobilized on Gold Nanoparticles
Current Pharmaceutical Biotechnology Structure Based Drug Design and Molecular Docking Studies of Anticancer Molecules Paclitaxel, Etoposide and Topotecan using Novel Ligands
Current Drug Discovery Technologies Preclinical Molecular Imaging of the Translocator Protein (TSPO) in a Metastases Model Based on Breast Cancer Xenografts Propagated in the Murine Brain
Current Molecular Medicine Fluorescent Substrates Useful as High Throughput Screening Tools for ADAM9
Combinatorial Chemistry & High Throughput Screening Modeling Anti-Allergic Natural Compounds by Molecular Topology
Combinatorial Chemistry & High Throughput Screening Cyclooxygenase-2 Inhibitors as a Therapeutic Target in Inflammatory Diseases
Current Medicinal Chemistry The Management of Metastatic Bone Disease with the Combination of Bisphosphonates and Radiotherapy: From Theory to Clinical Practice
Anti-Cancer Agents in Medicinal Chemistry