Abstract
We have synthesized a series of polyamine-based anilinoacridine derivatives. The preliminary biological evaluation indicated that the 9-anilinoacridine-polyamine derivatives had low or insignificant in vitro cytotoxicity against K562 cell line and K562/ADM, the drug-resistant cell line. However, the evaluation for P-gp modulation showed that they held potent P-gp inhibitory ability. Among them, the effect of compound 7c on P-gp was even greater than that of Verapamil, the known P-gp modulator. The results suggest that 9-anilinoacridine-polyamine derivatives can be employed as effective P-gp modulators.
Keywords: Anilinoacridine derivatives, cytotoxicity, multidrug resistance, P-glycoprotein, polyamine.
Medicinal Chemistry
Title:Synthesis and Preliminary Biological Evaluation of Polyamine-aniline Acridines as P-glycoprotein Inhibitors
Volume: 10 Issue: 5
Author(s): Jianhong Wang, Pengfei Cheng, Tianwei Luo, Zhaoyi Wang, Yahong Zhang and Jin Zhao
Affiliation:
Keywords: Anilinoacridine derivatives, cytotoxicity, multidrug resistance, P-glycoprotein, polyamine.
Abstract: We have synthesized a series of polyamine-based anilinoacridine derivatives. The preliminary biological evaluation indicated that the 9-anilinoacridine-polyamine derivatives had low or insignificant in vitro cytotoxicity against K562 cell line and K562/ADM, the drug-resistant cell line. However, the evaluation for P-gp modulation showed that they held potent P-gp inhibitory ability. Among them, the effect of compound 7c on P-gp was even greater than that of Verapamil, the known P-gp modulator. The results suggest that 9-anilinoacridine-polyamine derivatives can be employed as effective P-gp modulators.
Export Options
About this article
Cite this article as:
Wang Jianhong, Cheng Pengfei, Luo Tianwei, Wang Zhaoyi, Zhang Yahong and Zhao Jin, Synthesis and Preliminary Biological Evaluation of Polyamine-aniline Acridines as P-glycoprotein Inhibitors, Medicinal Chemistry 2014; 10 (5) . https://dx.doi.org/10.2174/15734064113096660052
DOI https://dx.doi.org/10.2174/15734064113096660052 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...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
-
Biology of Cox-2: An Application in Cancer Therapeutics
Current Drug Targets CDC25A and B Dual-Specificity Phosphatase Inhibitors: Potential Agents for Cancer Therapy
Current Medicinal Chemistry Therapeutic Strategies in Parkinsons Disease
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Radiolabelled Oligonucleotides for Imaging of Gene Expression with PET
Current Medicinal Chemistry APE1/Ref-1Role in Redox Signaling: Translational Applications of Targeting the Redox Function of the DNA Repair/Redox Protein APE1/Ref-1
Current Molecular Pharmacology Prostaglandin E<sub>2</sub> Receptor 4 (EP4): A Promising Therapeutic Target for the Treatment of Cancer and Inflammatory Diseases
Current Chemical Biology Aspartic Proteases in Drug Discovery
Current Pharmaceutical Design Targeted Protein Degradation: An Emerging Therapeutic Strategy in Cancer
Anti-Cancer Agents in Medicinal Chemistry Fusion of Wavelet and Morphological Features for Breast Cancer Diagnosis in Ultrasound Images
Current Medical Imaging Drug Targeting Systems for Cancer Therapy: Nanotechnological Approach
Mini-Reviews in Medicinal Chemistry Factors Associated with Pulmonary Embolism Recurrence and the Benefits of Long-term Anticoagulant Therapy
Cardiovascular & Hematological Disorders-Drug Targets The Potential Therapeutic Role of the HMGB1-TLR Pathway in Epilepsy
Current Drug Targets Inhibition of TGF- Signaling for the Treatment of Tumor Metastasis and Fibrotic Diseases
Current Signal Transduction Therapy Counter-Regulatory Role of Bile Acid Activated Receptors in Immunity and Inflammation
Current Molecular Medicine ABC Transporters as Potential Targets for Modulation of Drug Resistance
Mini-Reviews in Medicinal Chemistry Influence of Genetic Factors on the Development of Breast Cancer in the Older Woman
Current Aging Science Disruption of Circadian Rhythms and Sleep in Critical Illness: Potential Implications for Angiogenesis After Myocardial Infarction. A Review
Current Pharmaceutical Design Purinergic Receptors and Pain
Current Pharmaceutical Design Patents on Nanoparticulate Drug Delivery Systems - A Review
Recent Patents on Drug Delivery & Formulation Protective Effect of Isothiocyanates from Cruciferous Vegetables on Breast Cancer: Epidemiological and Preclinical Perspectives
Anti-Cancer Agents in Medicinal Chemistry