"Old Friends in New Guise": Exploiting Privileged Structures for Scaffold Re-Evolution/Refining

ISSN: 1875-5402 (Online)
ISSN: 1386-2073 (Print)

Volume 18, 10 Issues, 2015

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Combinatorial Chemistry & High Throughput Screening

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Rathnam Chaguturu
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Princeton Junction
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"Old Friends in New Guise": Exploiting Privileged Structures for Scaffold Re-Evolution/Refining

Combinatorial Chemistry & High Throughput Screening, 17(6): 536-553.

Author(s): Yu'ning Song, Wenmin Chen, Dongwei Kang, Qingzhu Zhang, Peng Zhan and Xinyong Liu.

Affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong, P.R. China.


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.


Drug design, drug repositioning, privileged structure, scaffold re-evolution, scaffold refining.

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Article Details

Volume: 17
Issue Number: 6
First Page: 536
Last Page: 553
Page Count: 18
DOI: 10.2174/1386207317666140122101631

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