{"id":{"repo_id":"uiuc","oai_identifier":"oai:www.ideals.illinois.edu:2142/84178"},"canonical_url":"https://search.dev.ndltd.org/etd/uiuc/oai:www.ideals.illinois.edu:2142/84178","repository":{"repo_id":"uiuc","name":"University of Illinois - Urbana-Champaign","base_url":"https://www.ideals.illinois.edu/oai-pmh"},"display":{"title":"Novel Core Scaffolds for the Development of Subtype Selective Estrogen Receptor Ligands","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.","abstract_html":"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.","abstract_has_math":false,"creators":["Compton, Dennis Ray"],"institution":"University of Illinois at Urbana-Champaign","degree_name":"Ph.D.","degree_level":"Dissertation","degree_discipline":"Chemistry","degree_department":null,"school":null,"contributors":["Katzenellenbogen, John A."],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2015,"date_issued":"2015-09-25T22:13:20Z","date_published":"2015-09-25T22:13:20Z","updated_at":"2026-07-22T22:26:22Z","subjects":["Chemistry, Organic"],"languages":["eng"],"rights":[],"rights_urls":[],"identifier_entries":[{"key":"dc:identifier","label":"Identifier","values":["(MiAaPQ)AAI3182441"],"render_values":[{"text":"(MiAaPQ)AAI3182441","href":null,"code":true}]}]},"links":{"outbound_url":"http://hdl.handle.net/2142/84178","outbound_label":"Handle","outbound_source":"dc:identifier"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:contributor","label":"Contributor","values":["Katzenellenbogen, John A."]},{"key":"dc:creator","label":"Author","values":["Compton, Dennis Ray"]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date","label":"Dc Date","values":["2015-09-25T22:13:20Z","10000-01-01","2005"]},{"key":"dc:type","label":"Dc Type","values":["text"]},{"key":"thesis:degree_discipline","label":"Discipline","values":["Chemistry"]},{"key":"thesis:degree_level","label":"Degree Level","values":["Dissertation"]},{"key":"thesis:degree_name","label":"Degree Name","values":["Ph.D."]},{"key":"thesis:institution_name","label":"Thesis Institution Name","values":["University of Illinois at Urbana-Champaign"]}]},{"id":"subjects_keywords","label":"Subjects and Keywords","entries":[{"key":"dc:subject","label":"Dc Subject","values":["Chemistry, Organic"]}]},{"id":"language_rights","label":"Language and Rights","entries":[{"key":"dc:language","label":"Dc Language","values":["eng"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier","label":"Identifier","values":["http://hdl.handle.net/2142/84178","(MiAaPQ)AAI3182441"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description","label":"Description","values":["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.","Made available in DSpace on 2015-09-25T22:13:20Z (GMT). No. of bitstreams: 2 license.txt: 4848 bytes, checksum: 96035ab3f5e1c23cc7138a224ce498bd (MD5) 3182441.pdf: 18856570 bytes, checksum: 8e7807cbc7031990e9bf077353171985 (MD5) Previous issue date: 2005","Embargo set by: Seth Robbins for item 85459 Lift date: Forever Reason: Restricted to the U of I community idenfinitely during batch ingest of legacy ETDs","Restricted to the U of I community idenfinitely during batch ingest of legacy ETDs","U of I Only","302 p.","Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 2005."]},{"key":"dc:title","label":"Title","values":["Novel Core Scaffolds for the Development of Subtype Selective Estrogen Receptor Ligands"]}]}],"canonical_facts":{"dc:contributor":["Katzenellenbogen, John A."],"dc:creator":["Compton, Dennis Ray"],"dc:date":["2015-09-25T22:13:20Z","10000-01-01","2005"],"dc:description":["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.","Made available in DSpace on 2015-09-25T22:13:20Z (GMT). No. of bitstreams: 2 license.txt: 4848 bytes, checksum: 96035ab3f5e1c23cc7138a224ce498bd (MD5) 3182441.pdf: 18856570 bytes, checksum: 8e7807cbc7031990e9bf077353171985 (MD5) Previous issue date: 2005","Embargo set by: Seth Robbins for item 85459 Lift date: Forever Reason: Restricted to the U of I community idenfinitely during batch ingest of legacy ETDs","Restricted to the U of I community idenfinitely during batch ingest of legacy ETDs","U of I Only","302 p.","Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 2005."],"dc:identifier":["http://hdl.handle.net/2142/84178","(MiAaPQ)AAI3182441"],"dc:language":["eng"],"dc:subject":["Chemistry, Organic"],"dc:title":["Novel Core Scaffolds for the Development of Subtype Selective Estrogen Receptor Ligands"],"dc:type":["text"],"thesis:degree_discipline":["Chemistry"],"thesis:degree_level":["Dissertation"],"thesis:degree_name":["Ph.D."],"thesis:institution_name":["University of Illinois at Urbana-Champaign"]},"updated_at":"2026-07-22T22:26:22Z"}