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
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
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
Can Dietary Polyphenols Prevent the Formation of Toxic Compounds from Maillard Reaction?
Current Drug Metabolism Cell Metabolism Under Microenvironmental Low Oxygen Tension Levels in Stemness, Proliferation and Pluripotency
Current Molecular Medicine Structural Design and Physicochemical Foundations of Hydrogels for Biomedical Applications
Current Medicinal Chemistry Chemotherapeutic Effects of Acridine Derivatives
Medicinal Chemistry Reviews - Online (Discontinued) Cubosomes: Versatile Nanosized Formulation for Efficient Delivery of Therapeutics
Current Drug Delivery Cytoplasmic CXCR4 High-Expression Exhibits Distinct Poor Clinicopathological Characteristics and Predicts Poor Prognosis in Triple-Negative Breast Cancer
Current Molecular Medicine The Effects of Bisphosphonates on the Bone Marrow Niche and Circulating and Disseminated Tumor Cells
Current Cancer Therapy Reviews Vitamins for Cancer Prevention and Treatment: An Insight
Current Molecular Medicine Purinergic Receptors and Pain
Current Pharmaceutical Design Clinical Molecular Imaging with PET Agents Other than 18F-FDG
Current Pharmaceutical Biotechnology Vitamin D and the Adaptive Immune System with Special Emphasis to Allergic Reactions and Allograft Rejection
Inflammation & Allergy - Drug Targets (Discontinued) Cellular and Physiological Effects of Ganoderma lucidum (Reishi)
Mini-Reviews in Medicinal Chemistry Role of Cytokines in Regulating Feeding Behaviour
Current Drug Targets Synthesis of [<sup>64</sup>Cu]Cu-NOTA-Bn-GE11 for PET Imaging of EGFR-Rich Tumors
Current Radiopharmaceuticals Organosulfur Compounds in Cancer Chemoprevention
Mini-Reviews in Medicinal Chemistry Adeno-Associated Virus-Mediated Gene Transfer in Hematopoietic Stem/Progenitor Cells as a Therapeutic Tool
Current Gene Therapy Novel Reverse-Phase High-Performance Liquid Chromatography (RPHPLC) Method for the Quantification of Apigenin in Ocimum Basilicum Linn Seeds (Tukmaria)
Current Analytical Chemistry Cerebral White Matter Injuries Following a Hypoxic/Ischemic Insult During the Perinatal Period: Pathophysiology, Prognostic Factors, and Future Strategy of Treatment Approach. A Minireview
Current Pharmaceutical Design Sulfotransferase 1A1 as a Biomarker for Susceptibility to Carcinogenesis: From Molecular Genetics to the Role of Dietary Flavonoids
Current Drug Metabolism Overcoming Cell Death and Tau Phosphorylation Mediated by PI3KInhibition: A Cell Assay to Measure Neuroprotection
CNS & Neurological Disorders - Drug Targets