Development of Combinatorial Approaches Towards Selective Estrogen Receptor Modulators: Investigations of Acyclic Amides and Tetra-Substituted Pyrazoles
Stauffer, Shaun Robert
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https://hdl.handle.net/2142/84460
Description
Title
Development of Combinatorial Approaches Towards Selective Estrogen Receptor Modulators: Investigations of Acyclic Amides and Tetra-Substituted Pyrazoles
Author(s)
Stauffer, Shaun Robert
Issue Date
1999
Doctoral Committee Chair(s)
Katzenellenbogen, John A.
Department of Study
Chemistry
Discipline
Chemistry
Degree Granting Institution
University of Illinois at Urbana-Champaign
Degree Name
Ph.D.
Degree Level
Dissertation
Keyword(s)
Chemistry, Biochemistry
Language
eng
Abstract
In addition, four basic side chain-containing pyrazoles that mimic potentially favorable orientations in the ER binding pocket were synthesized. Among the four sites for basic side chain incorporation, the C (5) piperidinylethoxy-substituted pyrazole was found to have the highest affinity and to be an ERalpha antagonist, blocking the action of E2 with a modest 10-fold potency selectivity over antagonism in ERbeta in in vitro reporter assays. This work illustrates the first efforts towards a novel SERM containing a pyrazole scaffold as its core structure.
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