Privileged Scaffolds for Library Design and Drug Discovery

By Matthew E. Welsch, S. Snyder, Brent R. Stockwell. Current Opinion in Chemical Biology, 2010

1,261 citations recorded by the source corpus.

This review explores the concept of using privileged scaffolds to identify biologically active compounds through building chemical libraries. We hope to accomplish three main objectives: to provide one of the most comprehensive listings of privileged scaffolds; to reveal through four selected examples the present state of the art in privileged scaffold library synthesis (in hopes of inspiring new and even more creative approaches); and also to offer some thoughts on how new privileged scaffolds might be identified and exploited.

Subfields: Molecular Biology, Organic Chemistry

View Paper: https://www.semanticscholar.org/paper/219f2cf58c5e952f9a16d619de1c0c58af068cd0

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In Molecular Biology

1. Brent R. Stockwell
2. Scott J. Dixon
3. Matthew E. Welsch
4. Nicholas P. Tatonetti
5. R. Kang
6. D. Tang
7. M. Conrad
8. James A. Olzmann

In Organic Chemistry

1. Matthew E. Welsch
2. Brent R. Stockwell

Citations in the corpus

• Pharmacological inhibition of cystine–glutamate exchange induces endoplasmic reticulum stress and ferroptosis (2014, background): “Erastin's quinazolinone core (Region A) is found in a number of biologically active compounds and is considered to be a ‘privileged’ scaffold (Welsch et al., 2010).”
• Single-electron transmetalation in organoboron cross-coupling by photoredox/nickel dual catalysis (2014, background): “A variety of nitrogen-containing heteroaryl bromides, classically challenging yet highly valued substrates as a result of their prevalence in biologically active compounds (27), performed well under the optimized reaction conditions.”