Abstract
A series of N10-substituted-2-methyl acridone derivatives are synthesized and are examined for its ability to reverse P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in breast cancer cell lines MCF-7 and MCF-7/Adr. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. The results showed that compound 16 with four carbon spacer exhibited promising in-vitro anti-cancer and reversal of drug resistance in comparison to the other analogues.
Keywords: Acridones, anti-cancer, P-glycoprotein (P-gp), multidrug resistance (MDR)
Medicinal Chemistry
Title: Synthesis of 2-Methyl N10-Substituted Acridones as Selective Inhibitors of Multidrug Resistance (MDR) Associated Protein in Cancer Cells
Volume: 4 Issue: 5
Author(s): Y. C. Mayur, Osman Ahmad, V. V.S. Rajendra Prasad, M. N. Purohit, N. Srinivasulu and S. M. Shanta Kumar
Affiliation:
Keywords: Acridones, anti-cancer, P-glycoprotein (P-gp), multidrug resistance (MDR)
Abstract: A series of N10-substituted-2-methyl acridone derivatives are synthesized and are examined for its ability to reverse P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in breast cancer cell lines MCF-7 and MCF-7/Adr. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. The results showed that compound 16 with four carbon spacer exhibited promising in-vitro anti-cancer and reversal of drug resistance in comparison to the other analogues.
Export Options
About this article
Cite this article as:
Mayur C. Y., Ahmad Osman, Rajendra Prasad V.S. V., Purohit N. M., Srinivasulu N. and Shanta Kumar M. S., Synthesis of 2-Methyl N10-Substituted Acridones as Selective Inhibitors of Multidrug Resistance (MDR) Associated Protein in Cancer Cells, Medicinal Chemistry 2008; 4 (5) . https://dx.doi.org/10.2174/157340608785700180
DOI https://dx.doi.org/10.2174/157340608785700180 |
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
-
High Expression of SIRT1 Associates with the Doxorubicin Resistance of Breast Cancer through the Activation of Akt
Anti-Cancer Agents in Medicinal Chemistry Role of Cervical Cancer Radiotherapy in the Expression of EGFR and p53 Gene
Current Proteomics The PYRIN Domain in Signal Transduction
Current Protein & Peptide Science An Update on Circumventing Multidrug Resistance in Cancer by Targeting P-Glycoprotein
Current Cancer Drug Targets Synthesis, Aromatase Inhibitory, Antiproliferative and Molecular Modeling Studies of Functionally Diverse D-Ring Pregnenolone Pyrazoles
Anti-Cancer Agents in Medicinal Chemistry Phosphonium Salt Displays Cytotoxic Effects Against Human Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry Postmenopausal Osteoporosis and Aerobic Exercise: A Review of the Literature
Current Rheumatology Reviews The BCL2-Family of Protein Ligands as Cancer Drugs: The Next Generation of Therapeutics
Current Medicinal Chemistry - Anti-Cancer Agents TNF alpha Inhibition as Treatment Modality for Certain Rheumatologic and Gastrointestinal Diseases
Endocrine, Metabolic & Immune Disorders - Drug Targets Hormone Replacement Therapy and Stroke
Current Vascular Pharmacology Neurological Disorders in Medical Use of <i>Cannabis</i>: An Update
CNS & Neurological Disorders - Drug Targets The Role of MRI in Treatment Planning for Rectal Cancer - A Review
Current Cancer Therapy Reviews Target-based Anti-angiogenic Therapy in Breast Cancer
Current Pharmaceutical Design Targeting Cytokines as an Approach to Modulate Allergic Diseases: The Clinical Experience
Medicinal Chemistry Reviews - Online (Discontinued) Synthesis, In Vitro Antitumor Activity and Molecular Mechanism of Novel Furan Derivatives and their Precursors
Anti-Cancer Agents in Medicinal Chemistry The Tumor Stroma as Mediator of Drug Resistance - A Potential Target to Improve Cancer Therapy?
Current Pharmaceutical Biotechnology Psychological Sequelae of Ovarian Cancer Screening and Genetic Testing for Ovarian Cancer Susceptibility
Current Women`s Health Reviews Molecular Imaging of Apoptosis with Radio-Labeled Annexin A5 Focused on the Evaluation of Tumor Response to Chemotherapy
Anti-Cancer Agents in Medicinal Chemistry Volumetric Analysis of the Hypothalamus, Amygdala and Hippocampus in Non-Suicidal and Suicidal Mood Disorder Patients – A Post-Mortem Study
CNS & Neurological Disorders - Drug Targets On the Power of Additional and Complex Chromosomal Aberrations in CML
Current Genomics