Abstract
A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calcium assay. Among synthesized and tested compounds, 4a showed the highest calcium overload preventing activity (IC50=39μM) and 7e demonstrated the highest calcium channel inhibiting activity (EC50=0.2 nM). Asymmetric ester 7a exerted both substantial calcium channel blocking and calcium overload preventing activity.
Keywords: Amlodipine, Asymmetric 1,4-dihydropyridines, Calcium channel antagonists, Cerebrocrast, Riodipine, 1,4-DHP, Calcium Level, Cardiovascular diseases, Varian Mercury, apoptosis, neuroprotective propertie, antihypertensive agents, NMR spectra, Aortic Ring Experiment
Letters in Drug Design & Discovery
Title: Calcium Level Controlling Activities of Novel Derivatives of Amlodipine,Riodipine and Cerebrocrast
Volume: 9 Issue: 3
Author(s): R. Vilskersts, B. Vigante, Z. Neidere, A. Krauze, I. Domracheva, L. Bekere, I. Shestakova, G. Duburs and M. Dambrova
Affiliation:
Keywords: Amlodipine, Asymmetric 1,4-dihydropyridines, Calcium channel antagonists, Cerebrocrast, Riodipine, 1,4-DHP, Calcium Level, Cardiovascular diseases, Varian Mercury, apoptosis, neuroprotective propertie, antihypertensive agents, NMR spectra, Aortic Ring Experiment
Abstract: A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calcium assay. Among synthesized and tested compounds, 4a showed the highest calcium overload preventing activity (IC50=39μM) and 7e demonstrated the highest calcium channel inhibiting activity (EC50=0.2 nM). Asymmetric ester 7a exerted both substantial calcium channel blocking and calcium overload preventing activity.
Export Options
About this article
Cite this article as:
Vilskersts R., Vigante B., Neidere Z., Krauze A., Domracheva I., Bekere L., Shestakova I., Duburs G. and Dambrova M., Calcium Level Controlling Activities of Novel Derivatives of Amlodipine,Riodipine and Cerebrocrast, Letters in Drug Design & Discovery 2012; 9 (3) . https://dx.doi.org/10.2174/157018012799129909
DOI https://dx.doi.org/10.2174/157018012799129909 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
![](/images/wayfinder.jpg)
- 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
-
Peptides or Small Molecules? Different Approaches to Develop More Effective CDK Inhibitors
Current Medicinal Chemistry Decreasing the Metastatic Potential in Cancers - Targeting the Heparan Sulfate Proteoglycans
Current Drug Targets Modulation of the Cannabinoid System: A New Perspective for the Treatment of the Alzheimer’s Disease
Current Neuropharmacology Apolipoprotein E-mediated Modulation of ADAM10 in Alzheimer's Disease
Current Alzheimer Research Immunological Approaches to Prevent Neuronal Apoptosis During Neuroinflammation
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Recent Advances in Hematopoietic Stem Cell-Mediated Regeneration
Recent Patents on Regenerative Medicine Aptamers: Selection, Modification and Application to Nervous System Diseases
Current Medicinal Chemistry The Development of MetAP-2 Inhibitors in Cancer Treatment
Current Medicinal Chemistry CB1 Cannabinoid Receptors and their Associated Proteins
Current Medicinal Chemistry The Role of Survivin for Radiation Oncology: Moving Beyond Apoptosis Inhibition
Current Medicinal Chemistry The “Aged Garlic Extract” (AGE) and One of its Active Ingredients S-Allyl-LCysteine (SAC) as Potential Preventive and Therapeutic Agents for Alzheimer's Disease (AD)
Current Medicinal Chemistry Lipid Nanoparticles as Vehicles for Macromolecules: Nucleic Acids and Peptides
Recent Patents on Drug Delivery & Formulation The Ubiquitous Choline Transporter SLC44A1
Central Nervous System Agents in Medicinal Chemistry miRNAs as Modulators of Cholesterol in Breast Cancer Stem Cells: An Approach to Overcome Drug Resistance in Cancer
Current Drug Targets The Synthetic Oleanane Triterpenoid HIMOXOL Induces Autophagy in Breast Cancer Cells via ERK1/2 MAPK Pathway and Beclin-1 Up-regulation
Anti-Cancer Agents in Medicinal Chemistry The Contribution of Proteinase-Activated Receptors to Intracellular Signaling, Transcellular Transport and Autophagy in Alzheimer´s Disease
Current Alzheimer Research Exploring the Mitochondrial Apoptotic Cell Death Landscape and Associated Components Serving as Molecular Targets, Primarily for Synthetic and Natural Drugs Targeting Oncology Therapeutics
Current Molecular Pharmacology Vascular Endothelial Growth Factor and Vascular Endothelial Growth Factor Receptor Inhibitors as Anti-Angiogenic Agents in Cancer Therapy
Recent Patents on Anti-Cancer Drug Discovery The Therapeutic Potential of RNA Interference: Novel Approaches for Cancer Treatment
Current Pharmaceutical Biotechnology Novel Therapeutic Approaches Based on the Targeting of Microenvironment-Derived Survival Pathways in Human Cancer: Experimental Models and Translational Issues
Current Pharmaceutical Design