Abstract
As commented by the Nobelist James Black that “The most fruitful basis of the discovery of a new drug is to start with an old drug”, drug repurposing represents an attractive drug discovery strategy. Despite the success of several repurposed drugs on the market, the ultimate therapeutic potential of a large number of non-cancer drugs is hindered during their repositioning due to various issues including the limited efficacy and intellectual property. With the increasing knowledge about the pharmacological properties and newly identified targets, the scaffolds of the old drugs emerge as a great treasure-trove towards new cancer drug discovery. In this review, we summarize the recent advances in the development of novel small molecules for cancer therapy by scaffold repurposing with highlighted examples. The relevant strategies, advantages, challenges and future research directions associated with this approach are also discussed.
Keywords: Drug repurposing, Scaffold repurposing, Structure-activity relationships (SARs), Drug discovery, Cancer therapeutics.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Scaffold Repurposing of Old Drugs Towards New Cancer Drug Discovery
Volume: 16 Issue: 19
Author(s): Haijun Chen, Jianlei Wu, Yu Gao, Haiying Chen and Jia Zhou
Affiliation:
Keywords: Drug repurposing, Scaffold repurposing, Structure-activity relationships (SARs), Drug discovery, Cancer therapeutics.
Abstract: As commented by the Nobelist James Black that “The most fruitful basis of the discovery of a new drug is to start with an old drug”, drug repurposing represents an attractive drug discovery strategy. Despite the success of several repurposed drugs on the market, the ultimate therapeutic potential of a large number of non-cancer drugs is hindered during their repositioning due to various issues including the limited efficacy and intellectual property. With the increasing knowledge about the pharmacological properties and newly identified targets, the scaffolds of the old drugs emerge as a great treasure-trove towards new cancer drug discovery. In this review, we summarize the recent advances in the development of novel small molecules for cancer therapy by scaffold repurposing with highlighted examples. The relevant strategies, advantages, challenges and future research directions associated with this approach are also discussed.
Export Options
About this article
Cite this article as:
Chen Haijun, Wu Jianlei, Gao Yu, Chen Haiying and Zhou Jia, Scaffold Repurposing of Old Drugs Towards New Cancer Drug Discovery, Current Topics in Medicinal Chemistry 2016; 16 (19) . https://dx.doi.org/10.2174/1568026616666160216155556
DOI https://dx.doi.org/10.2174/1568026616666160216155556 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Medicinal Chemistry Advancement in Life-Threatening Diseases
The current issue will highlight concise reports that specify ground-breaking insights, including the novel discovery of drug targets and their action mechanism or drugs of novel classes. These are projected to encourage medicinal chemistry future efforts to address the most challenging medical needs. The current issue highlights further efforts to ...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
- Announcements
Related Articles
-
Tachykinins and the Cardiovascular System
Current Drug Targets Mechanisms of Activation and Key Roles of SGK3 Under Physiological Conditions and in Prostate and Breast Cancer
Current Signal Transduction Therapy PI3K/Akt/mTOR Intracellular Pathway and Breast Cancer: Factors, Mechanism and Regulation
Current Pharmaceutical Design Epidemics of Obesity and Metabolic Disorders: Are Dietary Fats or Sugars Involved?
Current Nutrition & Food Science Challenging the Current Approaches to Multiple Myeloma-Related Bone Disease: From Bisphosphonates to Target Therapy
Current Cancer Drug Targets ATP-Binding Cassette Transporters at the Blood-Brain Barrier in Ischaemic Stroke
Current Pharmaceutical Design Ligand-Based Pharmacophore Modeling, Atom-Based 3D-QSAR and Molecular Docking Studies on Substituted Thiazoles and Thiophenes as Polo-Like Kinase 1 (Plk1) Inhibitors
Combinatorial Chemistry & High Throughput Screening Photo- and Sono-Dynamic Therapy: A Review of Mechanisms and Considerations for Pharmacological Agents Used in Therapy Incorporating Light and Sound
Current Pharmaceutical Design Mitochondrial Therapeutics for Cardioprotection
Current Pharmaceutical Design The Tachykinergic System as Avenues for Drug Intervention
Recent Patents on CNS Drug Discovery (Discontinued) Molecular Switch of AhR in Repression or Activation of Stem Cell Signaling
Current Signal Transduction Therapy Impact of Drug Metabolism/Pharmacokinetics and their Relevance Upon Taxus-based Drug Development
Current Drug Metabolism Role of Carboxypeptidase N Invasion and Migration in Breast Cancer
Anti-Cancer Agents in Medicinal Chemistry Ultrasound Assisted Synthesis of 3-(het)aryl Isocoumarin Derivatives and their in vitro Pharmacological Evaluation
Mini-Reviews in Medicinal Chemistry Subject Index to Volume 10
Current Medicinal Chemistry An Approach Towards the Quantitative Structure-Activity Relationships for Sulfamate-Based Estrone Sulfatase Inhibitors
Letters in Drug Design & Discovery Evaluation of the in vitro Antitumor Activity of Nanostructured Cyclotides in Polymers of Eudragit® L 100-55 and RS 30 D
Letters in Drug Design & Discovery Predicting Drug Metabolism Induction In Silico
Current Topics in Medicinal Chemistry Stem Cell Therapy for Ischaemic Stroke: Translation from Preclinical Studies to Clinical Treatment
CNS & Neurological Disorders - Drug Targets Cytokine Profile in Patients Infected with Anisakis simplex in Endemic Areas: Dietary Intervention with Polyphenols: A Working Hypothesis
Endocrine, Metabolic & Immune Disorders - Drug Targets