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Katzenellenbogen, John A. Stauffer, Shaun Robert 2015-09-25T22:14:37Z 2015-09-25T22:14:37Z 10000-01-01 1999 1999 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. Made available in DSpace on 2015-09-25T22:14:37Z (GMT). No. of bitstreams: 2 license.txt: 4848 bytes, checksum: 96035ab3f5e1c23cc7138a224ce498bd (MD5) 9953147.pdf: 10835218 bytes, checksum: ddddbd10aecfcb63a51fe6dd517c0dfd (MD5) Previous issue date: 1999 Embargo set by: Seth Robbins for item 85741 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 209 p. Thesis (Ph.D.)--University of Illinois at Urbana-Champaign, 1999. http://hdl.handle.net/2142/84460 (MiAaPQ)AAI9953147 eng Chemistry, Biochemistry Development of Combinatorial Approaches Towards Selective Estrogen Receptor Modulators: Investigations of Acyclic Amides and Tetra-Substituted Pyrazoles text Chemistry Chemistry University of Illinois at Urbana-Champaign Dissertation Ph.D.