Abstract
In 2000, Wyeth reported that the 3-quinolinecarbonitrile ring system was a template for EGFR inhibitors. It soon became apparent that the group at C-4 of this core was responsible for kinase selectivity. A 4-(2,4-dichloro-5- methoxyanilino) substituent provided potent inhibitors of Src, a non-receptor tyrosine kinase that plays a key role in cell signaling. One compound from this series, SKI-606, bosutinib, is currently in clinical trials for the treatment of cancer.
Keywords: 3-Quinolinecarbonitrile, kinase, Src, cancer, Abl, CML, SKI-606, bosutinib
Current Topics in Medicinal Chemistry
Title: Exploitation of the 3-Quinolinecarbonitrile Template for Src Tyrosine Kinase Inhibitors
Volume: 8 Issue: 10
Author(s): Diane H. Boschelli
Affiliation:
Keywords: 3-Quinolinecarbonitrile, kinase, Src, cancer, Abl, CML, SKI-606, bosutinib
Abstract: In 2000, Wyeth reported that the 3-quinolinecarbonitrile ring system was a template for EGFR inhibitors. It soon became apparent that the group at C-4 of this core was responsible for kinase selectivity. A 4-(2,4-dichloro-5- methoxyanilino) substituent provided potent inhibitors of Src, a non-receptor tyrosine kinase that plays a key role in cell signaling. One compound from this series, SKI-606, bosutinib, is currently in clinical trials for the treatment of cancer.
Export Options
About this article
Cite this article as:
Boschelli H. Diane, Exploitation of the 3-Quinolinecarbonitrile Template for Src Tyrosine Kinase Inhibitors, Current Topics in Medicinal Chemistry 2008; 8 (10) . https://dx.doi.org/10.2174/156802608784911653
DOI https://dx.doi.org/10.2174/156802608784911653 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Adaptogens—History and Future Perspectives
Adaptogens are pharmacologically active compounds or plant extracts that are associated with the ability to enhance the body’s stability against stress. The intake of adaptogens is associated not only with a better ability to adapt to stress and maintain or normalise metabolic functions but also with better mental and physical ...read more
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chronic Kidney Disease
The scope of the special thematic issue includes but not limited to the mechanism of chronic kidney disease (CKD), the treatment of renal fibrosis and early diagnosis of CKD and so on. We also welcome manuscripts from other scientific research area with respect to internal medicine. Cell death has been ...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
- Announcements
Related Articles
-
Notch-Associated MicroRNAs in Cancer
Current Drug Targets Plasma Proteins Interaction with Curcumin Nanoparticles: Implications in Cancer Therapeutics
Current Drug Metabolism On the Nature of the Tumor-Initiating Cell
Current Stem Cell Research & Therapy Cytokine/Antibody Complexes: An Emerging Class of Immunostimulants
Current Pharmaceutical Design Synergistic Interactions between GW8510 and Gemcitabine in an In Vitro Model of Pancreatic Cancer
Anti-Cancer Agents in Medicinal Chemistry Pharmacology of Sigma (σ) Receptor Ligands from a Behavioral Perspective
Current Pharmaceutical Design Targeting p53-MDM2 Interaction Using Small Molecule Inhibitors and the Challenges Needed to be Addressed
Current Drug Targets Lymphatic Targeting of Nanosystems for Anticancer Drug Therapy
Current Pharmaceutical Design Extracellular Matrix and Aberrant Signaling in Lung Carcinoma: Role of Fibronectin in the Control of Human Lung Carcinoma Cell Growth,Apoptosis and Resistance to Therapy
Current Signal Transduction Therapy A Review on Exploring the Opportunities of Polymer Drug Conjugated Systems for Targeted Cancer Treatment
Current Drug Delivery Microarray Technologies for Intracellular Kinome Analysis
Current Medicinal Chemistry The Role of Zinc in the Treatment of Taste Disorders
Recent Patents on Food, Nutrition & Agriculture Radioprotection of Normal Tissue to Improve Radiotherapy: The Effect of the Bowman Birk Protease Inhibitor
Current Medicinal Chemistry - Anti-Cancer Agents A Comprehensive Review on the Medicinal Importance; Biological and Therapeutic Efficacy of <i>Lagenaria siceraria</i> (Mol.) (Bottle Gourd) Standley Fruit
Current Topics in Medicinal Chemistry Lessons from Nature: Sources and Strategies for Developing AMPK Activators for Cancer Chemotherapeutics
Anti-Cancer Agents in Medicinal Chemistry Exploiting Internal Ribosome Entry Sites in Gene Therapy Vector Design
Current Gene Therapy Poly(lactic acid)-poly(ethylene oxide) Block Copolymers: New Directions in Self-Assembly and Biomedical Applications
Current Medicinal Chemistry Discovery and Development of Natural Products and their Derivatives as Photosensitizers for Photodynamic Therapy
Current Medicinal Chemistry Targeting Protein Phosphatases for the Treatment of Chronic Liver Disease
Current Drug Targets Second Generation Taxanes: from the Natural Framework to the Challenge of Drug Resistance
Current Medicinal Chemistry - Anti-Cancer Agents