Cited by 1,509Computational Drug Discovery MethodsChemical Synthesis and AnalysisSynthesis and biological activity

Privileged scaffolds for library design and drug discovery

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Welsch, Matthew E, Snyder, Scott A, Stockwell, Brent R·2010·Current Opinion in Chemical Biology

Abstract

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.

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Crossref · 10.1016/j.cbpa.2010.02.018

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  • The fragment binding elements in the authors' initial studies were selected based on their representation in drug-like molecules and were diverse in structure and physicochemical properties.

    “The fragment binding elements in our initial studies were selected based on their representation in drug-like molecules14 and were accordingly diverse in structure and physicochemical properties.”

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Authors
Welsch, M. E., Snyder, S. A., & Stockwell, B. R.
Affiliations
  • Columbia University (US)
  • Howard Hughes Medical Institute (US)
Corresponding author
  • Snyder, Scott A
  • Stockwell, Brent R
Venue
Current Opinion in Chemical Biology
Publisher
Elsevier BV
Published
2010-06
Volume
14
Issue
3
Pages
347-361
ISSN
1367-5931 (ISSN-L)
OpenAlex
W2162106505
Cited by
1,509
References
49
Citations by year
2026: 83 · 2025: 84 · 2024: 97 · 2023: 101 · 2022: 111 · 2021: 102 · 2020: 109 · 2019: 119 · 2018: 108 · 2017: 114 · 2016: 104 · 2015: 96 · 2014: 91 · 2013: 69 · 2012: 53
FWCI
5.29
Type
journal article
Language
en
Open access
Locations
  • Current Opinion in Chemical Biology (publishedVersion)
  • PubMed (publishedVersion)
  • PubMed Central (acceptedVersion)
Funders
  • Howard Hughes Medical Institute
  • Arnold and Mabel Beckman Foundation
  • Research Corporation for Science Advancement
  • Eli Lilly and Company
  • National Cancer Institute (RC2CA148308, R01CA097061)
  • National Institute of General Medical Sciences (R01GM084994, R01GM085081, R01-GM84994)
Topics
  • Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
  • Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
Keywords
privileged scaffolds, chemical libraries, library design, drug discovery, scaffold-based drug design, chemical library synthesis, bioactive compounds
MeSH terms
Pharmaceutical Preparations, Humans, Models, Chemical, Protein Binding, Drug Delivery Systems, Receptors, Cytoplasmic and Nuclear, Small Molecule Libraries, Drug Discovery

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