Scaffold repurposing of old drugs towards new cancer drug discovery

Haijun Chen, Jianlei Wu, Yu Gao, Haiying Chen, Jia Zhou

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)2107-2114
Number of pages8
JournalCurrent topics in medicinal chemistry
Issue number19
StatePublished - Aug 1 2016


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

ASJC Scopus subject areas

  • Drug Discovery


Dive into the research topics of 'Scaffold repurposing of old drugs towards new cancer drug discovery'. Together they form a unique fingerprint.

Cite this