| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 7803122 | European Journal of Medicinal Chemistry | 2011 | 10 Pages |
Abstract
⺠Salicylaldoxime pseudocycle proves to be an efficient bioisosteric replacement of phenol. ⺠Improved selective binding to ER-beta is obtained by structural optimization of salicylaldoximes. ⺠Chloro/fluoro-substituted Salaldox B members show a binding affinity for ER-beta similar to that of estradiol. ⺠The best ER-beta ligands confirm their beta-selective full agonist properties. ⺠Docking analysis indicates a peculiar H-bond formation with Thr299 of ER-beta.
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Authors
Simone Bertini, Andrea De Cupertinis, Carlotta Granchi, Barbara Bargagli, Tiziano Tuccinardi, Adriano Martinelli, Marco Macchia, Jillian R. Gunther, Kathryn E. Carlson, John A. Katzenellenbogen, Filippo Minutolo,