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.
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