Abstract
5-Aryl-pyrrolo[2,3-d]pyrimidines incorporating different N7-substituents have been prepared and evaluated for their inhibitory potency towards the tyrosine kinase c-Src. Optimization of these compounds resulted in highly potent c-Src inhibitors, some (e.g. 4g, 6g, 7h, 8l ) with excellent specificity towards other receptor and nonreceptor tyrosine kinases. In addition compounds 4g, 5b and 5c are characterized by a good pharmacokinetic profile.
Keywords: tyrosine kinase inhibitor, c-src inhibitor
Mini-Reviews in Medicinal Chemistry
Title: N7-Substituted-5-aryl-pyrrolo[2,3-d]pyrimidines Represent a Versatile Class of Potent Inhibitors of the Tyrosine Kinase c-Src
Volume: 2 Issue: 3
Author(s): Eva Altmann, Leo Widler and Martin Missbach
Affiliation:
Keywords: tyrosine kinase inhibitor, c-src inhibitor
Abstract: 5-Aryl-pyrrolo[2,3-d]pyrimidines incorporating different N7-substituents have been prepared and evaluated for their inhibitory potency towards the tyrosine kinase c-Src. Optimization of these compounds resulted in highly potent c-Src inhibitors, some (e.g. 4g, 6g, 7h, 8l ) with excellent specificity towards other receptor and nonreceptor tyrosine kinases. In addition compounds 4g, 5b and 5c are characterized by a good pharmacokinetic profile.
Export Options
About this article
Cite this article as:
Altmann Eva, Widler Leo and Missbach Martin, N7-Substituted-5-aryl-pyrrolo[2,3-d]pyrimidines Represent a Versatile Class of Potent Inhibitors of the Tyrosine Kinase c-Src, Mini-Reviews in Medicinal Chemistry 2002; 2 (3) . https://dx.doi.org/10.2174/1389557023406188
DOI https://dx.doi.org/10.2174/1389557023406188 |
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
-
Age-Related Argonaute Loading of Ribosomal RNA Fragments
MicroRNA Effect of Boswellia serrata on Rat Trachea Contractility In Vitro
The Natural Products Journal Teaching Pharmacogenetics in Low and Middle Income Countries (LMICs): An Empirical Study of the Lessons Learned
Current Pharmacogenomics and Personalized Medicine HLA-G and Inflammatory Diseases
Inflammation & Allergy - Drug Targets (Discontinued) Editor’s Perspective: Metabolomics Currently
Current Metabolomics NO to Breast: When, Why and Why Not?
Current Pharmaceutical Design Bcl-2 Family Proteins as Therapeutic Targets
Current Pharmaceutical Design Development of HIV Reservoir Targeted Long Acting Nanoformulated Antiretroviral Therapies
Current Medicinal Chemistry The Nitric Oxide Prodrug JS-K and Its Structural Analogues as Cancer Therapeutic Agents
Anti-Cancer Agents in Medicinal Chemistry Genistein as a Potential Anticancer Agent Against Head and Neck Squamous Cell Carcinoma
Current Topics in Medicinal Chemistry Natural Flora and Anticancer Regime: Milestones and Roadmap
Anti-Cancer Agents in Medicinal Chemistry Radiolabeled Compounds in Diagnosis of Infectious and Inflammatory Disease
Current Pharmaceutical Design Medicinal Chemistry of P2X Receptors: Agonists and Orthosteric Antagonists
Current Medicinal Chemistry The Role of PET/CT and SPECT/CT in Oncology Drug Development
Current Molecular Imaging (Discontinued) Oleamide Derivatives are Prototypical Anti-Metastasis Drugs that Act by Inhibiting Connexin 26
Current Drug Safety IL-17 and its Receptor Complex as Therapeutic Targets in Arthritis
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Rational Combination of Targeted Therapies As A Strategy to Overcome The Mechanisms of Resistance to Inhibitors of EGFR Signaling
Current Pharmaceutical Design The β 2-Adrenergic Agonist Salbutamol Inhibits Migration, Invasion and Metastasis of the Human Breast Cancer MDA-MB- 231 Cell Line
Current Cancer Drug Targets Status of Programmed Death Ligand 1 (PD-L1) by Immunohistochemistry and Scoring Algorithms
Current Drug Targets Vasoactive Factors and Diabetic Retinopathy: Vascular Endothelial Growth Factor, Cycoloxygenase-2 and Nitric Oxide
Current Pharmaceutical Design