Files in this item



application/pdf3182441.pdf (19MB)Restricted to U of Illinois
(no description provided)PDF


Title:Novel Core Scaffolds for the Development of Subtype Selective Estrogen Receptor Ligands
Author(s):Compton, Dennis Ray
Doctoral Committee Chair(s):Katzenellenbogen, John A.
Department / Program:Chemistry
Degree Granting Institution:University of Illinois at Urbana-Champaign
Subject(s):Chemistry, Organic
Abstract:We have explored many novel core scaffolds, heterocyclic and acyclic, in our search for subtype selective ligands. During our studies we discovered ligands containing new pharmacological profiles for estrogens. The pyrazolo[1,5-a]pyrimidine ligands provided us with two new pharmacological classes of ligands: (1) ERbeta potency selective antagonists and (2) ERbeta potency and efficacy selective antagonists. These ligands provide researchers with the ability to selectively antagonize ERbeta allowing for them to study the effects of ERbeta inhibition in cells, in the presence of ERalpha. Although these are interesting ligands we desired to develop an ERbeta potency selective agonist. An ERbeta selective agonist will allow researchers to study the role of ERbeta when activated. To aid in the development of ERbeta selective agonists we described a pharmacophore model that we believed would aid in ligand design. Using this model we developed a series of ERbeta potency and efficacy selective agonists. The new pharmacological profiles of estrogens that we have developed will provide researchers with additional tools to study and elucidate the role of the estrogen receptor.
Issue Date:2005
Description:302 p.
Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 2005.
Other Identifier(s):(MiAaPQ)AAI3182441
Date Available in IDEALS:2015-09-25
Date Deposited:2005

This item appears in the following Collection(s)

Item Statistics