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Title:Development of Combinatorial Approaches Towards Selective Estrogen Receptor Modulators: Investigations of Acyclic Amides and Tetra-Substituted Pyrazoles
Author(s):Stauffer, Shaun Robert
Doctoral Committee Chair(s):Katzenellenbogen, John A.
Department / Program:Chemistry
Discipline:Chemistry
Degree Granting Institution:University of Illinois at Urbana-Champaign
Degree:Ph.D.
Genre:Dissertation
Subject(s):Chemistry, Biochemistry
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.
Issue Date:1999
Type:Text
Language:English
Description:209 p.
Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 1999.
URI:http://hdl.handle.net/2142/84460
Other Identifier(s):(MiAaPQ)AAI9953147
Date Available in IDEALS:2015-09-25
Date Deposited:1999


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