Abstract
Paullones are a class of molecules structurally based on the 7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one parent scaffold. Many of these structures are inhibitors of certain protein kinases, namely cyclin-dependent kinases and glycogen synthase kinase-3. Being well referenced in the literature on the one hand and commercially available on the other hand, paullones have been used as biochemical tools in basic research and drug development for more than a decade. This review gives an overview over the published reports regarding chemistry, biological activity and pharmacological applications of paullone derivatives.
Keywords: Azepinones, cyclin dependent kinases, GSK-3, indoles, paullones, protein kinase inhibitors, cancer, glycogen synthase kinase-3, screening project, antiproliferative activity, COMPARE, chemotypes inhibiting cyclin-dependent kinases (CDKs)
Current Topics in Medicinal Chemistry
Title: Paullones as Inhibitors of Protein Kinases
Volume: 11 Issue: 11
Author(s): Nadine Tolle and Conrad Kunick
Affiliation:
Keywords: Azepinones, cyclin dependent kinases, GSK-3, indoles, paullones, protein kinase inhibitors, cancer, glycogen synthase kinase-3, screening project, antiproliferative activity, COMPARE, chemotypes inhibiting cyclin-dependent kinases (CDKs)
Abstract: Paullones are a class of molecules structurally based on the 7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one parent scaffold. Many of these structures are inhibitors of certain protein kinases, namely cyclin-dependent kinases and glycogen synthase kinase-3. Being well referenced in the literature on the one hand and commercially available on the other hand, paullones have been used as biochemical tools in basic research and drug development for more than a decade. This review gives an overview over the published reports regarding chemistry, biological activity and pharmacological applications of paullone derivatives.
Export Options
About this article
Cite this article as:
Tolle Nadine and Kunick Conrad, Paullones as Inhibitors of Protein Kinases, Current Topics in Medicinal Chemistry 2011; 11 (11) . https://dx.doi.org/10.2174/156802611795589601
DOI https://dx.doi.org/10.2174/156802611795589601 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Modulation of ABC Transporters by Nuclear Receptors: Physiological, Pathological and Pharmacological Aspects
Current Medicinal Chemistry Proteomics Analysis of Trastuzumab Toxicity in the H9c2 Cardiomyoblast Cell Line and its Inhibition by Carvedilol
Current Pharmaceutical Biotechnology Safety of Cabergoline in the Management of Pituitary Prolactin-Induced Symptoms with Patients Treated with Atypical Neuroleptics
Current Drug Safety Current Evidence and Potential Mechanisms of Therapeutic Action of PEDF in Cervical Cancer Treatment
Current Molecular Medicine Prostaglandin E2 Receptors as Potential Bone Anabolic Targets – Selective EP4 Receptor Agonists
Current Molecular Pharmacology Molecular Replacement in Cancer Therapy: Reversing Cancer Metabolic and Mitochondrial Dysfunction, Fatigue and the Adverse Effects of Cancer Therapy
Current Cancer Therapy Reviews Advances in α(v)β(3) Integrin-Targeting Cancer Therapy and Imaging with Radiolabeled RGD Peptides
Current Radiopharmaceuticals Benzocoumarins: Isolation, Synthesis, and Biological Activities
Mini-Reviews in Medicinal Chemistry Aquaporin Biology and Nervous System
Current Neuropharmacology A Novel Multiple Tyrosine-kinase Targeted Agent to Explore the Future Perspectives of Anti-Angiogenic Therapy for the Treatment of Multiple Solid Tumors: Cabozantinib
Anti-Cancer Agents in Medicinal Chemistry Cognitive Functions under Anti-HER2 Targeted Therapy in Cancer Patients: A Scoping Review
Endocrine, Metabolic & Immune Disorders - Drug Targets The Ubiquitous Choline Transporter SLC44A1
Central Nervous System Agents in Medicinal Chemistry Influence of New Synthetic Xanthones on the Proliferation and Migration Potential of Cancer Cell Lines In Vitro
Anti-Cancer Agents in Medicinal Chemistry Macrophage Flipping from Foe to Friend: A Matter of Interest in Breast Carcinoma Heterogeneity Driving Drug Resistance
Current Cancer Drug Targets Peripheral TRPV1 Receptors As Targets for Drug Development: New Molecules and Mechanisms
Current Pharmaceutical Design Lab-on-a-chip Dielectrophoretic Manipulation of Beta-2 Microglobulin for Toxin Removal in An Artificial Kidney
Micro and Nanosystems Breast Cancer Stem Cells and Intrinsic Subtypes: Controversies Rage On
Current Stem Cell Research & Therapy Possible Consequences of Blocking Transient Receptor Potential Vanilloid 1
Current Pharmaceutical Biotechnology Prevention of Cancer in the Upper Gastrointestinal Tract with COX-Inhibition. Still an Option?
Current Pharmaceutical Design Estimation of specific activity of 177Lu by `saturation assay` principle using DOTA as ligand
Current Radiopharmaceuticals