Development of Combinatorial Approaches Towards Selective Estrogen Receptor Modulators: Investigations of Acyclic Amides and Tetra-Substituted Pyrazoles

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.

Name thesis:degree_name

Ph.D.

Level thesis:degree_level

Dissertation

Discipline thesis:degree_discipline

Chemistry

Grantor

University of Illinois at Urbana-Champaign

Year dc:date

2015

Author dc:creator

• Stauffer, Shaun Robert

Contributors dc:contributor

• Katzenellenbogen, John A.

• Chemistry, Biochemistry

Language dc:language

eng

Identifier

(MiAaPQ)AAI9953147

OAI identifier oai:identifier

oai:www.ideals.illinois.edu:2142/84460