Ontology highlight
ABSTRACT:
SUBMITTER: Hwang JY
PROVIDER: S-EPMC2753520 | biostudies-literature | 2009 Jul
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20090701 13
We have previously reported the discovery and preliminary structure activity relationships of a series of beta-aminoketones that disrupt the binding of coactivators to TR. However, the most active compounds had moderate inhibitory potency and relatively high cytotoxicity, resulting in narrow therapeutic index. Additionally, preliminary evaluation of in vivo toxicology revealed a significant dose related cardiotoxicity. Here we describe the improvement of pharmacological properties of thyroid hor ...[more]