Submit Manuscript  

Article Details

Scaffold Repurposing of Old Drugs Towards New Cancer Drug Discovery

[ Vol. 16 , Issue. 19 ]


Haijun Chen, Jianlei Wu, Yu Gao, Haiying Chen and Jia Zhou   Pages 2107 - 2114 ( 8 )


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.


Drug repurposing, Scaffold repurposing, Structure-activity relationships (SARs), Drug discovery, Cancer therapeutics.


College of Chemistry, Fuzhou University, Fuzhou, Fujian 350108, China., Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, United States.

Graphical Abstract:

Read Full-Text article