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
-
Selected Heterocyclic Compounds as Antioxidants. Synthesis and Biological Evaluation
Current Topics in Medicinal Chemistry Cognitive Functions under Anti-HER2 Targeted Therapy in Cancer Patients: A Scoping Review
Endocrine, Metabolic & Immune Disorders - Drug Targets PDGF-D Signaling: A Novel Target in Cancer Therapy
Current Drug Targets SPECT-CT in Radiotherapy Planning, with Main Reference to Patients with Breast Cancer
Current Radiopharmaceuticals Antibody Targeting of TGF-β in Cancer Patients
Current Pharmaceutical Biotechnology Enzymatic Properties and Physiological Roles of Cytosolic 5’-Nucleotidase II.
Current Medicinal Chemistry Pharmacogenomics of the Human ATP-Binding Cassette Transporter ABCG2
Current Pharmacogenomics Directed Differentiation of Pluripotent Cells Towards Therapeutic Stem Cells
Recent Patents on Regenerative Medicine Effects of Polymorphisms of the CYP450 Enzyme Genes on Estrogen Status and the Risk for Osteoporosis
Current Pharmacogenomics Design, Synthesis, Cytotoxic Activity and Apoptosis-inducing Action of Novel Cinnoline Derivatives as Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Use of Anti-Cancer Drugs, Mitocans, to Enhance the Immune Responses against Tumors
Current Pharmaceutical Biotechnology A Network-Based Cancer Drug Discovery: From Integrated Multi-Omics Approaches to Precision Medicine
Current Pharmaceutical Design Doxycycline in Mitochondrial Mediated Pathway of Apoptosis: A Systematic Review
Anti-Cancer Agents in Medicinal Chemistry Design and Synthesis of Novel Thiosemicarbazones as Potent Anti-breast Cancer Agents
Letters in Drug Design & Discovery Impact of Viscosity and Refractive Index on Droplet Size and Zeta Potential of Model O/W and W/O Nanoemulsion
Current Nanoscience Application of Microdialysis in Clinical Pharmacology
Current Clinical Pharmacology Integrins in Pulmonary Inflammatory Diseases
Current Pharmaceutical Design Will Pharmacogenetics Predict Response to Therapies in Rheumatoid Arthritis?
Current Pharmacogenomics Approaches for Developing Novel Microtubule Targeting Agents (MTAs) for Therapeutic Exploitation
Current Pharmaceutical Design Novel Insights Into c-Src
Current Pharmaceutical Design