The attempts to increase novel drug productivity through creative discovery technologies have fallen short of
producing the satisfactory results. For these reasons, evolved from the concept of drug repositioning, “privileged
structure”-guided scaffold re-evolution/refining is a primary strategy to identify structurally novel chemotypes by
modifying the central core structure and the side-chain of the existing active compounds, or to exploit undescribed
bioactivites by making full use of readily derivatized motifs with well-established synthetic protocols. Herein, we review
the basic tricks of exploiting privileged structures for scaffold re-evolution/refining. The power of this strategy is
exemplified in the discovery of other new therapeutic applications by refining privileged structures in anti-viral agents.
Keywords: Drug design, drug repositioning, privileged structure, scaffold re-evolution, scaffold refining.
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