Discovery of covalent modifiers via the complexity to diversity strategy
Sawyer, Adam Michael
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https://hdl.handle.net/2142/110875
Description
Title
Discovery of covalent modifiers via the complexity to diversity strategy
Author(s)
Sawyer, Adam Michael
Issue Date
2021-04-29
Director of Research (if dissertation) or Advisor (if thesis)
Hergenrother, Paul J
Department of Study
Chemistry
Discipline
Chemistry
Degree Granting Institution
University of Illinois at Urbana-Champaign
Degree Name
M.S.
Degree Level
Thesis
Keyword(s)
Covalent modifiers
targeted covalent inhibitors
complexity to diversity
complex molecule synthesis
Abstract
Targeted covalent drugs have recently become integral parts of drug discovery. Given the advantages of high-throughput screening in drug discovery, many electrophilic fragment collections have been developed as a promising alternative to discover and validate novel targets. However, most covalent screening libraries consist of flat, low molecular weight compounds that are lacking in complexity and are incapable of addressing more complex targets, such as protein-protein interactions. To fill this gap, a library of 19 complex and diverse compounds containing electrophilic moieties has been synthesized and screened for anticancer activity in cell culture. The results from these studies suggest the potential for electrophilic natural product-like compounds to be used in the investigation of biological targets implicated in cancer.
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