Abstract
Among the family of nitrogen-containing heterocycles, quinoxalinone (or quinoxalin-2-one) core, characterized by pyrazin-2(1H)-one fused to benzene ring at two adjacent carbon atoms, has been frequently found in a variety of pharmacologically active compounds with biological or pharmaceutical applications. It was gratifying that a larger part of these bioactive quinoxalinone-based derivatives has entered various clinical trials, which in turn hastens the synthetic versatility and also initiates various derivatization of quinoxalinone scaffold. In this review, we highlighted the newly emerged quinoxalinone- based derivatives or analogues, with the emphasis of their biological applications and structure-activity analysis covering literatures in recent years.
Keywords: Binding mode, biological activities, derivates, quinoxaline, quinoxalinone skeleton, SAR analysis.
Mini-Reviews in Medicinal Chemistry
Title:Quinoxalinone as a Privileged Platform in Drug Development
Volume: 18 Issue: 5
Author(s): Leilei Shi, Wei Hu, Jifeng Wu, Huaiyu Zhou, Hua Zhou and Xun Li*
Affiliation:
- Key Laboratory of Chemistry and Chemical Biology (Ministry of Education), Department of Pharmaceutical Science, College of Pharmacy, Shandong University, Jinan,China
Keywords: Binding mode, biological activities, derivates, quinoxaline, quinoxalinone skeleton, SAR analysis.
Abstract: Among the family of nitrogen-containing heterocycles, quinoxalinone (or quinoxalin-2-one) core, characterized by pyrazin-2(1H)-one fused to benzene ring at two adjacent carbon atoms, has been frequently found in a variety of pharmacologically active compounds with biological or pharmaceutical applications. It was gratifying that a larger part of these bioactive quinoxalinone-based derivatives has entered various clinical trials, which in turn hastens the synthetic versatility and also initiates various derivatization of quinoxalinone scaffold. In this review, we highlighted the newly emerged quinoxalinone- based derivatives or analogues, with the emphasis of their biological applications and structure-activity analysis covering literatures in recent years.
Export Options
About this article
Cite this article as:
Shi Leilei, Hu Wei , Wu Jifeng , Zhou Huaiyu, Zhou Hua and Li Xun*, Quinoxalinone as a Privileged Platform in Drug Development, Mini-Reviews in Medicinal Chemistry 2018; 18 (5) . https://dx.doi.org/10.2174/1389557517666171101111134
DOI https://dx.doi.org/10.2174/1389557517666171101111134 |
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
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...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
- 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
-
Biology and Therapeutic Applications of Peroxisome Proliferator- Activated Receptors
Current Topics in Medicinal Chemistry The Neuroprotective Role of PEDF: Implication for the Therapy of Neurological Disorders
Current Molecular Medicine The Retinoblastoma Tumour Suppressor in Model Organisms-New Insights from Flies and Worms
Current Molecular Medicine Potentials of Hydrogels in Cancer Therapy
Current Cancer Therapy Reviews PTD/CPP Peptide-Mediated Delivery of siRNAs
Current Pharmaceutical Design Stem Cells: In Sickness and in Health
Current Stem Cell Research & Therapy Differential Expression of miR-20a and miR-145 in Colorectal Tumors as Potential Location-specific miRNAs
MicroRNA Differential Binding Preference of Methylpheophorbide a and Its Diboronated Derivatives to Albumin and Low Density Lipoproteins
Anti-Cancer Agents in Medicinal Chemistry Tea (Camellia sinensis (L.)): A Putative Anticancer Agent in Bladder Carcinoma?
Anti-Cancer Agents in Medicinal Chemistry Recent Progress in Research on Ribosome Inactivating Proteins
Current Protein & Peptide Science Management of Incidental Findings in the Era of Next-generation Sequencing
Current Genomics Intracellular Delivery of Potential Therapeutic Genes: Prospects in Cancer Gene Therapy
Current Gene Therapy The Mad2-Binding Protein p31<sup>comet</sup> as a Potential Target for Human Cancer Therapy
Current Cancer Drug Targets RNA Interference as Therapeutics for Hepatocellular Carcinoma
Recent Patents on Anti-Cancer Drug Discovery Advances in Oncolytic Virus Therapy for Glioma
Recent Patents on CNS Drug Discovery (Discontinued) MicroRNAs - Key Players in Haematopoiesis
Current Signal Transduction Therapy Curcumin and Curcumin-like Molecules: From Spice to Drugs
Current Medicinal Chemistry Multi-Kinase Inhibitors
Current Medicinal Chemistry Instructions from the Vascular System - Directing Neural Stem Cell Fate in Health and Disease
Current Medicinal Chemistry Nuclear Export as a Novel Therapeutic Target: The CRM1 Connection
Current Cancer Drug Targets