Ontology highlight
ABSTRACT:
SUBMITTER: Gryder BE
PROVIDER: S-EPMC3812312 | biostudies-literature | 2013 Jul
REPOSITORIES: biostudies-literature
Gryder Berkley E BE Rood Michael K MK Johnson Kenyetta A KA Patil Vishal V Raftery Eric D ED Yao Li-Pan D LP Rice Marcie M Azizi Bahareh B Doyle Donald F DF Oyelere Adegboyega K AK
Journal of medicinal chemistry 20130703 14
We describe a set of novel histone deacetylase inhibitors (HDACi) equipped with either an antagonist or an agonist of the estrogen receptor (ER) to confer selective activity against breast cancers. These bifunctional compounds potently inhibit HDAC at nanomolar concentrations and either agonize or antagonize ERα and ERβ. The ER antagonist activities of tamoxifen-HDACi conjugates (Tam-HDACi) are nearly identical to those of tamoxifen. Conversely, ethynyl-estradiol-HDACi conjugates (EED-HDACi) hav ...[more]