Abstract
The MDR chemosensitising activity of several analogues of the ardeemins, including five derivatives of the ABCD fragment, nine derivatives of the complete hexacyclic framework and one seco analogue lacking the B ring was studied. The results obtained confirm that the pharmacophoric moiety of the ardeemins as MDR reversers is located at their DEF fragment, and suggest that the epimer of the ardeemins at the alanine stereocenter should be more active than the natural stereoisomer.
Keywords: Antitumour drug resistance, MDR, glycoprotein P-170, ardeemin, pharmacophore
Letters in Drug Design & Discovery
Title: MDR Reversal by Deprenylated Tetracyclic and Hexacyclic Analogues of N-Acetylardeemin: Confirmation of the Ardeemin Pharmacophore
Volume: 3 Issue: 6
Author(s): Carmen Avendano, Esmeralda Caballero, Cristina Mendez-Vidal, Ana R. de Quesada and J. Carlos Menendez
Affiliation:
Keywords: Antitumour drug resistance, MDR, glycoprotein P-170, ardeemin, pharmacophore
Abstract: The MDR chemosensitising activity of several analogues of the ardeemins, including five derivatives of the ABCD fragment, nine derivatives of the complete hexacyclic framework and one seco analogue lacking the B ring was studied. The results obtained confirm that the pharmacophoric moiety of the ardeemins as MDR reversers is located at their DEF fragment, and suggest that the epimer of the ardeemins at the alanine stereocenter should be more active than the natural stereoisomer.
Export Options
About this article
Cite this article as:
Avendano Carmen, Caballero Esmeralda, Mendez-Vidal Cristina, de Quesada R. Ana and Carlos Menendez J., MDR Reversal by Deprenylated Tetracyclic and Hexacyclic Analogues of N-Acetylardeemin: Confirmation of the Ardeemin Pharmacophore, Letters in Drug Design & Discovery 2006; 3 (6) . https://dx.doi.org/10.2174/157018006777805558
DOI https://dx.doi.org/10.2174/157018006777805558 |
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
-
The Role of STAT3 Signaling in Mediating Tumor Resistance to Cancer Therapy
Current Drug Targets Liposomes as Versatile Platform for Cancer Theranostics: Therapy, Bio-imaging, and Toxicological Aspects
Current Pharmaceutical Design Retinoid Receptors in Inflammatory Responses: A Potential Target for Pharmacology
Current Drug Targets - Inflammation & Allergy Effects of Anticancer Drugs in Reproductive Parameters of Juvenile Male Animals and Role of Protective Agents
Anti-Cancer Agents in Medicinal Chemistry Exploiting Protein Phosphatase Inhibitors Based on Cantharidin Analogues for Cancer Drug Discovery
Mini-Reviews in Medicinal Chemistry Pharmacogenomics: The Influence of Genomic Variation on Drug Response
Current Topics in Medicinal Chemistry Plasmid-Mediated Muscle-Targeted Gene Therapy for Circulating Therapeutic Protein Replacement: A Tale of the Tortoise and the Hare?
Current Gene Therapy Targeting of Leukemia-Initiating Cells to Develop Curative Drug Therapies: Straightforward but Nontrivial Concept
Current Cancer Drug Targets Fibroblast Growth Factor Receptor (FGFR): A New Target for Non-small Cell Lung Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Targeting mTOR Pathways in Human Malignancies
Current Pharmaceutical Design The Involvement of Heat Shock Proteins and Related Molecules in the Resistance to Therapies in Breast and Gynecologic Cancer
Current Cancer Therapy Reviews Population Diversity and its Relationship with Infectious and Tumor Diseases
Current Immunology Reviews (Discontinued) Modulation of TRAIL-Induced Apoptosis by HDAC Inhibitors
Current Cancer Drug Targets miRNAs as Modulators of Cholesterol in Breast Cancer Stem Cells: An Approach to Overcome Drug Resistance in Cancer
Current Drug Targets Implications of FLT3 Mutations in the Therapy of Acute Myeloid Leukemia
Reviews on Recent Clinical Trials Chalcones in Cancer: Understanding their Role in Terms of QSAR. II Part
Mini-Reviews in Medicinal Chemistry New Treatment Approaches in Acute Myeloid Leukemia: Review of Recent Clinical Studies
Reviews on Recent Clinical Trials Molecular Advances Toward the Understanding of the Patho-Biology of Idiopathic Myelofibrosis
Current Immunology Reviews (Discontinued) What Western Pharmacists Need to Know About Traditional Chinese Medicine; A Canadian Perspective
Current Traditional Medicine Editorial Review of 2012
Current Radiopharmaceuticals