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 |
![](/images/wayfinder.jpg)
- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
-
Opinion Paper: Promise and Pragmatism in Clinical Microbiome Research
Mini-Reviews in Medicinal Chemistry Synthesis and Biomedical Applications of Dendrimers
Current Organic Chemistry Tumor-Derived Exosomes Contain microRNAs with Immunological Function: Implications for a Novel Immunosuppression Mechanism
MicroRNA Application of Targeted Therapy to Malignant Gliomas and Response to Treatment
Current Signal Transduction Therapy Flavonoids and the Brain: Evidences and Putative Mechanisms for a Protective Capacity
Current Neuropharmacology Transcription Factors in Asthma: Are Transcription Factors a New Target for Asthma Therapy?
Current Drug Targets The Complex Biology of FOXO
Current Drug Targets Targeting the Nuclear Transport Machinery by Rational Drug Design
Current Pharmaceutical Design Targeting Nodal and Cripto-1: Perspectives Inside Dual Potential Theranostic Cancer Biomarkers
Current Medicinal Chemistry Indolealkylamines from Toad Vertebrates and Sea Invertebrates - Their Identification and Potential Activities on the Central Nervous System
Central Nervous System Agents in Medicinal Chemistry A Review on Exploring Better Safety Prospects in Managing Cancer using Liposomal Combinations of Food Bioactive Compounds and Anticancer Drugs: Combisomes
Current Drug Delivery Detection of Lysyl Oxidase-Like 2 (LOXL2), a Biomarker of Metastasis from Breast Cancers Using Human Blood Samples
Recent Patents on Biomarkers Laboratory Techniques for Human Viral Encephalitis Diagnosis
Infectious Disorders - Drug Targets Regulation of HIF-1α at the Transcriptional Level
Current Pharmaceutical Design Large-Scale Production Means for the Manufacturing of Lentiviral Vectors
Current Gene Therapy Subject Index to Volume 4
Current Cancer Drug Targets Cellular Antiviral Factors that Target Particle Infectivity of HIV-1
Current HIV Research In Vitro, In Vivo and In Silico Analysis of the Anticancer and Estrogen-like Activity of Guava Leaf Extracts
Current Medicinal Chemistry Erythropoietin: Cytoprotection in Vascular and Neuronal Cells
Current Drug Targets - Cardiovascular & Hematological Disorders Targeting Focal Adhesion Kinase in Neuroblastoma
Anti-Cancer Agents in Medicinal Chemistry