Highly selective salicylketoxime-based estrogen receptor β agonists display antiproliferative activities in a glioma model.

ABSTRACT: Estrogen receptor β (ERβ) selective agonists are considered potential therapeutic agents for a variety of pathological conditions, including several types of cancer. Their development is particularly challenging, since differences in the ligand binding cavities of the two ER subtypes α and β are minimal. We have carried out a rational design of new salicylketoxime derivatives which display unprecedentedly high levels of ERβ selectivity for this class of compounds, both in binding affinity and in cell-based functional assays. An endogenous gene expression assay was used to further characterize the pharmacological action of these compounds. Finally, these ERβ-selective agonists were found to inhibit proliferation of a glioma cell line in vitro. Most importantly, one of these compounds also p

SUBMITTER: Paterni I 

PROVIDER: S-EPMC4610302 | biostudies-literature | 2015 Feb

REPOSITORIES: biostudies-literature