Abstract
The attempts to increase novel drug productivity through creative discovery technologies have fallen short of producing the satisfactory results. For these reasons, evolved from the concept of drug repositioning, “privileged structure”-guided scaffold re-evolution/refining is a primary strategy to identify structurally novel chemotypes by modifying the central core structure and the side-chain of the existing active compounds, or to exploit undescribed bioactivites by making full use of readily derivatized motifs with well-established synthetic protocols. Herein, we review the basic tricks of exploiting privileged structures for scaffold re-evolution/refining. The power of this strategy is exemplified in the discovery of other new therapeutic applications by refining privileged structures in anti-viral agents.
Keywords: Drug design, drug repositioning, privileged structure, scaffold re-evolution, scaffold refining.
Combinatorial Chemistry & High Throughput Screening
Title:"Old Friends in New Guise": Exploiting Privileged Structures for Scaffold Re-Evolution/Refining
Volume: 17 Issue: 6
Author(s): Yu'ning Song, Wenmin Chen, Dongwei Kang, Qingzhu Zhang, Peng Zhan and Xinyong Liu
Affiliation:
Keywords: Drug design, drug repositioning, privileged structure, scaffold re-evolution, scaffold refining.
Abstract: The attempts to increase novel drug productivity through creative discovery technologies have fallen short of producing the satisfactory results. For these reasons, evolved from the concept of drug repositioning, “privileged structure”-guided scaffold re-evolution/refining is a primary strategy to identify structurally novel chemotypes by modifying the central core structure and the side-chain of the existing active compounds, or to exploit undescribed bioactivites by making full use of readily derivatized motifs with well-established synthetic protocols. Herein, we review the basic tricks of exploiting privileged structures for scaffold re-evolution/refining. The power of this strategy is exemplified in the discovery of other new therapeutic applications by refining privileged structures in anti-viral agents.
Export Options
About this article
Cite this article as:
Song Yu'ning, Chen Wenmin, Kang Dongwei, Zhang Qingzhu, Zhan Peng and Liu Xinyong, "Old Friends in New Guise": Exploiting Privileged Structures for Scaffold Re-Evolution/Refining, Combinatorial Chemistry & High Throughput Screening 2014; 17 (6) . https://dx.doi.org/10.2174/1386207317666140122101631
DOI https://dx.doi.org/10.2174/1386207317666140122101631 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to 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
-
Curcumin: A Natural Pan-HDAC Inhibitor in Cancer
Current Pharmaceutical Design Cancer Vaccines in Phase II/III Clinical Trials: State of the Art and Future Perspectives
Current Cancer Drug Targets Organic Cation Transporters: Physiology, Toxicology and Special Focus on Ethidium as a Novel Substrate
Current Drug Metabolism Systemic and Biophase Bioavailability and Pharmacokinetics of Nanoparticulate Drug Delivery Systems
Current Drug Delivery Apoptosis-Inducing Effects of Amaryllidaceae Alkaloids
Current Medicinal Chemistry Radioprotective Effects of Plants from the Lamiaceae Family
Anti-Cancer Agents in Medicinal Chemistry Treatment of Helicobacter pylori Infection in Children
Current Pharmaceutical Design Thermodynamics and Electro-Biologic Prospects for Therapies to Intervene in Cancer Progression
Current Cancer Therapy Reviews Synthesis of 9-O-3-(1-piperazinyl/morpholinyl/piperidinyl)pentyl-berberines as Potential Antioxidant and Cytotoxic Agents
Anti-Cancer Agents in Medicinal Chemistry Epigenetic Basis of Neuronal and Synaptic Plasticity
Current Topics in Medicinal Chemistry Low Content of Protein S29 in Ribosomes of Human Lung Cancer Cell Line A549: Detected by Twodimensional Electrophoresis
Protein & Peptide Letters Nanosuspensions - An Update on Recent Patents, Methods of Preparation, and Evaluation Parameters
Recent Patents on Nanotechnology Potential Cancer Gene Therapy by Baculoviral Transduction
Current Gene Therapy Microenvironment and Brain Tumor Stem Cell Maintenance: Impact of the Niche
Anti-Cancer Agents in Medicinal Chemistry Cardioprotective Effects of Natural Products <i>via</i> the Nrf2 Signaling Pathway
Current Vascular Pharmacology From a Better Understanding of the Mechanisms of Action of Histone Deacetylases Inhibitors to the Progress of the Treatment of Malignant Lymphomas and Plasma Cell Myeloma
Recent Patents on Anti-Cancer Drug Discovery Abatacept and Glomerular Diseases: The Open Road for the Second Signal as a New Target is Settled Down
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery The Venom of the Centipede Scolopendra subspinipes mutilans Inhibits the Growth of Myelogenous Leukemia Cell Lines
Letters in Drug Design & Discovery Editorial: Pulmonary Involvement in Systemic Disorders
Current Drug Targets - Inflammation & Allergy Natural and Structure-based RXR Ligand Scaffolds and Their Functions
Current Topics in Medicinal Chemistry