Abstract
With the successful use of gefitinib and erlotinib in clinic, some potent EGFR tyrosine kinase receptor inhibitors have gained widespread concern in the treatment of ovarian or non-small-cell lung cancer. However, the emergence of EGFR-activating mutations resist to the drugs, there is an impending need to design new inhibitor targeted EGFR. Furthermore, the understanding of mutual effect between EGFR and drug has been available, it has become a hot spot for the research of anticancer drugs. We have designed and synthesized a series of 6-methoxy-7-(3-morpholinopropoxy)-1-(2- phenoxyethyl)-quinoxalin-2(1H)-one derivatives as novel EGFR inhibitors. Most of the compounds have showed inhibitory activity toward EGFR kinase. This work has demonstrated it is possible to construct a new type of EGFR protein kinase inhibitor using a designin strategy.
Keywords: Anticancer, EGFR inhibitor, kinase assay, molecular docking, quinazolin-2(1H)-one, tyrosine kinase.
Anti-Cancer Agents in Medicinal Chemistry
Title:Design, Synthesis and Biological Evaluation of Quinoxalin-2(1H)-one Derivatives as EGFR Tyrosine Kinase Inhibitors
Volume: 15 Issue: 2
Author(s): Xuemei Qin, Xiao Han, Liming Hu, Zhipeng Li, Zhufeng Geng, Zhanyang Wang, Chengchu Zeng and Xiangqian Xiao
Affiliation:
Keywords: Anticancer, EGFR inhibitor, kinase assay, molecular docking, quinazolin-2(1H)-one, tyrosine kinase.
Abstract: With the successful use of gefitinib and erlotinib in clinic, some potent EGFR tyrosine kinase receptor inhibitors have gained widespread concern in the treatment of ovarian or non-small-cell lung cancer. However, the emergence of EGFR-activating mutations resist to the drugs, there is an impending need to design new inhibitor targeted EGFR. Furthermore, the understanding of mutual effect between EGFR and drug has been available, it has become a hot spot for the research of anticancer drugs. We have designed and synthesized a series of 6-methoxy-7-(3-morpholinopropoxy)-1-(2- phenoxyethyl)-quinoxalin-2(1H)-one derivatives as novel EGFR inhibitors. Most of the compounds have showed inhibitory activity toward EGFR kinase. This work has demonstrated it is possible to construct a new type of EGFR protein kinase inhibitor using a designin strategy.
Export Options
About this article
Cite this article as:
Qin Xuemei, Han Xiao, Hu Liming, Li Zhipeng, Geng Zhufeng, Wang Zhanyang, Zeng Chengchu and Xiao Xiangqian, Design, Synthesis and Biological Evaluation of Quinoxalin-2(1H)-one Derivatives as EGFR Tyrosine Kinase Inhibitors, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (2) . https://dx.doi.org/10.2174/187152061502150116173357
DOI https://dx.doi.org/10.2174/187152061502150116173357 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Apoptosis Induction by Erucylphosphohomocholine via the 18 kDa Mitochondrial Translocator Protein: Implications for Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry Natural Bioactive Compounds as Emerging Therapeutic Molecules Against Breast Cancer: Emphasis on the Role of Phytoestrogens
Current Drug Targets Vitamin D and miRNAs in Cancer
Current Gene Therapy Zebrafish: Predictive Model for Targeted Cancer Therapeutics from Nature
Current Cancer Drug Targets Quantization of Angiogenesis and Image Analysis
Current Angiogenesis (Discontinued) 4,6-diaryl Pyrimidones as Constrained Chalcone Analogues: Design, Synthesis and Evaluation as Antiproliferative Agents
Anti-Cancer Agents in Medicinal Chemistry PI3K Inhibitors for Cancer Therapy: What has been Achieved So Far?
Current Medicinal Chemistry Immunoregulatory and Effector Activities of Nitric Oxide and Reactive Nitrogen Species in Cancer
Current Medicinal Chemistry One Pot Green Synthesis of Doxorubicin and Curcumin Loaded Magnetic Nanoparticles and Cytotoxicity Studies
Anti-Cancer Agents in Medicinal Chemistry Discovery of P3971 an Orally Efficacious Novel Anticancer Agent Targeting HIF-1α and STAT3 Pathways
Anti-Cancer Agents in Medicinal Chemistry 18F-fluoro-deoxy-D-glucose PET/CT in Establishing the Relationship Between the Metabolic Activity of Aorta and Iliac Artery Aneurysms in Cancer Patients
Current Medical Imaging Anti-Tumor Activity of Non-Nucleosidic Reverse Transcriptase Inhibitors
Current Pharmaceutical Design Recent Advances in the Development of Selective Mcl-1 Inhibitors for the Treatment of Cancer (2017-Present)
Recent Patents on Anti-Cancer Drug Discovery Personalized Medicine, Bioethics and Social Responsibilities: Re-thinking the Pharmaceutical Industry to Remedy Inequities in Patient Care and International Health
Current Pharmacogenomics and Personalized Medicine The Role of IRF1 and IRF2 Transcription Factors in Leukaemogenesis
Current Gene Therapy Endoplasmic Reticulum Stress, Calcium Dysregulation and Altered Protein Translation: Intersection of Processes That Contribute to Cancer Cachexia Induced Skeletal Muscle Wasting
Current Drug Targets Chemodiversity in Freshwater and Terrestrial Cyanobacteria – A Source for Drug Discovery
Current Drug Targets MDA-7/IL-24-Based Cancer Gene Therapy: Translation from the Laboratory to the Clinic
Current Gene Therapy New Molecular Targets in the Treatment of NSCLC
Current Pharmaceutical Design Journey Describing the Cytotoxic Potential of Withanolides: A Patent Review
Recent Patents on Anti-Cancer Drug Discovery