Abstract
Kinases are probably the most important signaling enzymes, which represent about 20% of the druggable genome. Currently, more than 150 kinases are known. So, kinase inhibition therapy has become a very important area of drug research since most of our diseases are related to intra or intercellular signaling by kinases. Indole alkaloids are extensively studied for their biological activities in several pharmaceutical areas, including, for example, antitumor. Among this chemical family, indolinone displays very promising antitumor properties by inhibiting various kinase families. These small molecules have a low molecular weight and most of them bind to protein kinases competing with ATP for the ATP-binding site. This review focuses on the indolinone based drugs approved for the treatment of cancer, drugs under clinical trial and then chemical diversity of various synthetic analogues of indolinone and their metabolites as various kinase inhibitors. This review also focused on structural activity relationship (SAR), mechanisms of action and biological targets through which indolinone and its derivatives display their antitumor activity.
Keywords: Anticancer, growth factor, indole, inhibitor, isatin, Kinase, antitumor, immunodeficiency, phosphorylation, endothelial, ploidy, Angiogenesis, TrkA Inhibitor
Mini-Reviews in Medicinal Chemistry
Title: Indolinones as Promising Scaffold as Kinase Inhibitors: A Review
Volume: 12 Issue: 2
Author(s): C. R. Prakash and S. Raja
Affiliation:
Keywords: Anticancer, growth factor, indole, inhibitor, isatin, Kinase, antitumor, immunodeficiency, phosphorylation, endothelial, ploidy, Angiogenesis, TrkA Inhibitor
Abstract: Kinases are probably the most important signaling enzymes, which represent about 20% of the druggable genome. Currently, more than 150 kinases are known. So, kinase inhibition therapy has become a very important area of drug research since most of our diseases are related to intra or intercellular signaling by kinases. Indole alkaloids are extensively studied for their biological activities in several pharmaceutical areas, including, for example, antitumor. Among this chemical family, indolinone displays very promising antitumor properties by inhibiting various kinase families. These small molecules have a low molecular weight and most of them bind to protein kinases competing with ATP for the ATP-binding site. This review focuses on the indolinone based drugs approved for the treatment of cancer, drugs under clinical trial and then chemical diversity of various synthetic analogues of indolinone and their metabolites as various kinase inhibitors. This review also focused on structural activity relationship (SAR), mechanisms of action and biological targets through which indolinone and its derivatives display their antitumor activity.
Export Options
About this article
Cite this article as:
R. Prakash C. and Raja S., Indolinones as Promising Scaffold as Kinase Inhibitors: A Review, Mini-Reviews in Medicinal Chemistry 2012; 12 (2) . https://dx.doi.org/10.2174/138955712798995039
DOI https://dx.doi.org/10.2174/138955712798995039 |
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
-
mTOR: A Novel Therapeutic Target for Diseases of Multiple Systems
Current Drug Targets Gallium-68 in Medical Imaging
Current Radiopharmaceuticals Flavopiridol, the First Cyclin-Dependent Kinase Inhibitor: Recent Advances in Combination Chemotherapy
Mini-Reviews in Medicinal Chemistry Dual Role of S100A8 and S100A9 in Inflammation-Associated Cancer
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Src Family Nonreceptor Tyrosine Kinases as Molecular Targets for Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry High Throughput Screening of Normal and Neoplastic Tissue Samples
Combinatorial Chemistry & High Throughput Screening Nanostructural Hybrid Sensitizers for Photodynamic Therapy
Current Pharmaceutical Design Molecular Replacement in Cancer Therapy: Reversing Cancer Metabolic and Mitochondrial Dysfunction, Fatigue and the Adverse Effects of Cancer Therapy
Current Cancer Therapy Reviews Targeted Delivery of Bleomycin: A Comprehensive Anticancer Review
Current Cancer Drug Targets Genetic Polymorphisms of Drug Metabolising Enzymes and Drug Transporters in Relation to Cancer Risk
Current Cancer Therapy Reviews Recent Advances in Optical Cancer Imaging of EGF Receptors
Current Medicinal Chemistry Comparative Analysis of Current Modality of Therapy in Head and Neck Squamous Cell Carcinoma Correlating the Expression Level of p38α
Current Cancer Therapy Reviews Herpes Simplex Encephalitis: From Virus to Therapy
Infectious Disorders - Drug Targets Recent Developments in the Field of Tumor-Inhibiting Metal Complexes
Current Pharmaceutical Design Synthesis and Preliminary Evaluation of 5-[18F]fluoroleucine
Current Radiopharmaceuticals Fluorine-18 Labeled Amino Acids for Oncologic Imaging with Positron Emission Tomography
Current Topics in Medicinal Chemistry Current Issues in the Utility of Blood Oxygen Level Dependent MRI for the Assessment of Modulations in Tumor Oxygenation
Current Medical Imaging Characterization of Stem-Like Cells Directly Isolated from Freshly Resected Laryngeal Squamous Cell Carcinoma Specimens
Current Stem Cell Research & Therapy Therapeutic Use of Snake Venom Components: A Voyage from Ancient to Modern India
Mini-Reviews in Organic Chemistry Editorial (Thematic issue: Discovering New Anticancer Activities from Old Drugs)
Current Medicinal Chemistry