Abstract
Vascular endothelial growth factor receptor (VEGFR) is an important receptor tyrosine kinase (RTK) in the induction of angiogenesis. Abnormal activation of VEGFR leads to several disorders including cancer. Nowadays, inhibition of VEGFR kinase has been one of the most powerful clinical strategies in cancer treatment and great efforts to design and synthesize small molecular VEGFR inhibitors for cancer research have been made in recent years. This review highlights the major progress and development of them, including their structure and pharmacophore features, biological activities and structure-activity relationships (SAR). Special attentions are paid to the compounds available in market or in advanced clinical stages.
Keywords: Vascular endothelial growth factor receptor, anticancer, inhibitor, angiogenesis, small molecular, VEGF, PlGF, Receptor Tyrosine Kinase, multiple myeloma, hematopoiesis, autophosphorylation, Quinazolines, Quinolines, Vandetanib, NSCLC, 1, PD-153035, Cediranib, KRN633, KRN951, Ki 8751, Valatanib, 12, AAL-993, 13, AMG 706, Phthalazines, Anthranilamides, Oxindoles, Sunitinib, GIST, RCC, Semaxanib, FGFR, AEE788, HUVEC, renal cell carcinoma, Sorafenib, Pazopanib, Axitinib, BMS-605541, X-ray crystallography, molecular modeling assay, VEGFR kinase
Mini-Reviews in Medicinal Chemistry
Title: Recent Progress of Small Molecular VEGFR Inhibitors as Anticancer Agents
Volume: 11 Issue: 1
Author(s): D. Xu, T.-L. Wang, L.-P. Sun and Q.-D. You
Affiliation:
Keywords: Vascular endothelial growth factor receptor, anticancer, inhibitor, angiogenesis, small molecular, VEGF, PlGF, Receptor Tyrosine Kinase, multiple myeloma, hematopoiesis, autophosphorylation, Quinazolines, Quinolines, Vandetanib, NSCLC, 1, PD-153035, Cediranib, KRN633, KRN951, Ki 8751, Valatanib, 12, AAL-993, 13, AMG 706, Phthalazines, Anthranilamides, Oxindoles, Sunitinib, GIST, RCC, Semaxanib, FGFR, AEE788, HUVEC, renal cell carcinoma, Sorafenib, Pazopanib, Axitinib, BMS-605541, X-ray crystallography, molecular modeling assay, VEGFR kinase
Abstract: Vascular endothelial growth factor receptor (VEGFR) is an important receptor tyrosine kinase (RTK) in the induction of angiogenesis. Abnormal activation of VEGFR leads to several disorders including cancer. Nowadays, inhibition of VEGFR kinase has been one of the most powerful clinical strategies in cancer treatment and great efforts to design and synthesize small molecular VEGFR inhibitors for cancer research have been made in recent years. This review highlights the major progress and development of them, including their structure and pharmacophore features, biological activities and structure-activity relationships (SAR). Special attentions are paid to the compounds available in market or in advanced clinical stages.
Export Options
About this article
Cite this article as:
Xu D., Wang T.-L., Sun L.-P. and You Q.-D., Recent Progress of Small Molecular VEGFR Inhibitors as Anticancer Agents, Mini-Reviews in Medicinal Chemistry 2011; 11 (1) . https://dx.doi.org/10.2174/138955711793564015
DOI https://dx.doi.org/10.2174/138955711793564015 |
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
-
Transposable Elements in Cancer and Other Human Diseases
Current Cancer Drug Targets LRP/LR as an Alternative Promising Target in Therapy of Prion Diseases, Alzheimers Disease and Cancer
Infectious Disorders - Drug Targets Humoral Immunity in HIV-1 Exposure: Cause or Effect of HIV Resistance?
Current HIV Research Smart Drug Release Systems Based on Stimuli-Responsive Polymers
Mini-Reviews in Medicinal Chemistry Proteomics in Acute Myelogenous Leukaemia (AML): Methodological Strategies and Identification of Protein Targets for Novel Antileukaemic Therapy
Current Drug Targets Developing Histone Deacetylase Inhibitors as Anti-Cancer Therapeutics
Current Medicinal Chemistry N6-Methyladenosine-Related RNA Signature Predicting the Prognosis of Ovarian Cancer
Recent Patents on Anti-Cancer Drug Discovery Energy Dependent Transport of Xenobiotics and Its Relevance to Multidrug Resistance
Current Cancer Drug Targets Adult Neural Stem Cell Therapy: Expansion In Vitro, Tracking In Vivo and Clinical Transplantation
Current Drug Targets Bladder Cancer Stem Cells
Current Stem Cell Research & Therapy Autophagy Driven Extracellular Vesicles in the Leukaemic Microenvironment
Current Cancer Drug Targets Perspectives for Novel Mixed Diruthenium-Organic Drugs as Metallopharmaceuticals in Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry New Insights into the Molecular Resistance Mechanisms of Chronic Myeloid Leukemia
Current Cancer Drug Targets Epigenetic Interventions Increase the Radiation Sensitivity of Cancer Cells
Current Pharmaceutical Design Chlorambucil Cytotoxicity Reduction in Rats Through Bone Marrow, An In vivo Study
Anti-Cancer Agents in Medicinal Chemistry Identification of Novel Potent Inhibitors Against Bcl-xL Anti-apoptotic Protein Using Docking Studies
Protein & Peptide Letters Interleukin-15 in Gene Therapy of Cancer
Current Gene Therapy Metal-N-Heterocyclic Carbene Complexes as Anti-Tumor Agents
Current Medicinal Chemistry Targeted Therapy for Advanced Urothelial Cancer of the Bladder: Where Do We Stand?
Anti-Cancer Agents in Medicinal Chemistry Obesity Modulation - The Role in Carcinogenesis
Anti-Cancer Agents in Medicinal Chemistry