Abstract
Background & Method: In this ongoing research, it is aimed to investigate the synthesis, structure identification and effects on urokinase-type plasminogen activators (uPA) and its receptor levels of 4-(3H-imidazo[4,5-b]pyridin-2-yl)-N-substituted benzamide and benzamidine derivatives. uPA levels obtained from 4b and 7d administration were similar to 5-FU (5-fluorouracil) for colorectal carcinoma cells (p<0.05). 4b and 7d significantly reduced uPAR (urokinase-type plasminogen activator receptor) levels on both cell lines (p<0.05).
Conclusion: uPAR levels obtaining from 4b and 7d administration were similar to 5-FU for both cell lines colorectal (Colo205, CCL-222) and hepatocellular (HepG2, CCL-23) carcinoma cells (p<0.05).
Keywords: Imidazopyridine, benzamide, benzamidine, urinary plasminogen activator, uPAR, upamostat.
Mini-Reviews in Medicinal Chemistry
Title:Benzamide and Benzamidine Compounds as New Inhibitors of Urokinasetype Plasminogen Activators
Volume: 18 Issue: 20
Author(s): Canan Kuş*, Ezgi Özer, Yeşim Korkmaz, Erkan Yurtcu and Rukiye Dağalp
Affiliation:
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100-Tandogan, Ankara,Turkey
Keywords: Imidazopyridine, benzamide, benzamidine, urinary plasminogen activator, uPAR, upamostat.
Abstract: Background & Method: In this ongoing research, it is aimed to investigate the synthesis, structure identification and effects on urokinase-type plasminogen activators (uPA) and its receptor levels of 4-(3H-imidazo[4,5-b]pyridin-2-yl)-N-substituted benzamide and benzamidine derivatives. uPA levels obtained from 4b and 7d administration were similar to 5-FU (5-fluorouracil) for colorectal carcinoma cells (p<0.05). 4b and 7d significantly reduced uPAR (urokinase-type plasminogen activator receptor) levels on both cell lines (p<0.05).
Conclusion: uPAR levels obtaining from 4b and 7d administration were similar to 5-FU for both cell lines colorectal (Colo205, CCL-222) and hepatocellular (HepG2, CCL-23) carcinoma cells (p<0.05).
Export Options
About this article
Cite this article as:
Kuş Canan *, Özer Ezgi , Korkmaz Yeşim, Yurtcu Erkan and Dağalp Rukiye , Benzamide and Benzamidine Compounds as New Inhibitors of Urokinasetype Plasminogen Activators, Mini-Reviews in Medicinal Chemistry 2018; 18 (20) . https://dx.doi.org/10.2174/1389557518666180816110740
DOI https://dx.doi.org/10.2174/1389557518666180816110740 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
-
Advances in Drug Safety
Current Pharmaceutical Design Breast Cancer Classification Using Discrete Wavelet Transformation and Deep Learning
Recent Advances in Computer Science and Communications Editorial (Thematic issue: Discovering New Anticancer Activities from Old Drugs)
Current Medicinal Chemistry Breast Cancer Resistance Protein: A Potential Therapeutic Target for Cancer
Current Drug Targets Vascular Endothelial Growth Factor: A New Paradigm for Targeting Various Diseases
Current Angiogenesis (Discontinued) Advancements within Modern Machine Learning Methodology: Impacts and Prospects in Biomarker Discovery
Current Medicinal Chemistry Design of Zein Conjugation and Surface Modification for Targeting Drug Delivery
Current Drug Targets Facile Synthesis of Hollow Mesoporous Hydroxyapatite Nanoparticles for Intracellular Bio-imaging
Current Nanoscience Lactate Transporters and pH Regulation: Potential Therapeutic Targets in Glioblastomas
Current Cancer Drug Targets Prognostic and Predictive Biomarkers in Cancer
Current Cancer Drug Targets Nanomedicine as a Strategy for Natural Compound Delivery to Prevent and Treat Cancers
Current Pharmaceutical Design Aqueous Extract of Arbutus unedo Inhibits STAT1 Activation in Human Breast Cancer Cell Line MDA-MB-231 and Human Fibroblasts Through SHP2 Activation
Medicinal Chemistry Novel Kynurenic Acid Analogues in the Treatment of Migraine and Neurodegenerative Disorders: Preclinical Studies and Pharmaceutical Design
Current Pharmaceutical Design Apoptosis Following Photodynamic Tumor Therapy: Induction, Mechanisms and Detection
Current Pharmaceutical Design Development of a Sensitive Cost-Effective Capture ELISA for Detection of Murine Monoclonal Antibodies - Correlation with SPR Biosensor Technology
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers
Current Medicinal Chemistry YB-1 Protein and Multidrug Resistance of Tumor Cells
Current Signal Transduction Therapy Editorials (Pharmacogenomics in Primary Care: A Crucial Entry Point for Global Personalized Medicine?)
Current Pharmacogenomics and Personalized Medicine Folate Based Radiopharmaceuticals for Imaging and Therapy of Cancer and Inflammation
Current Pharmaceutical Design Aptamers as Targeting Delivery Devices or Anti-cancer Drugs for Fighting Tumors
Current Drug Metabolism