Ontology highlight
ABSTRACT:
SUBMITTER: Hwang JY
PROVIDER: S-EPMC3308170 | biostudies-literature | 2012 Mar
REPOSITORIES: biostudies-literature
Hwang Jong Yeon JY Attia Ramy R RR Zhu Fangyi F Yang Lei L Lemoff Andrew A Jeffries Cynthia C Connelly Michele C MC Guy R Kiplin RK
Journal of medicinal chemistry 20120223 5
We previously identified a series of methylsulfonylnitrobenzoates (MSNBs) that block the interaction of the thyroid hormone receptor with its coactivators. MSNBs inhibit coactivator binding through irreversible modification of cysteine 298 of the thyroid hormone receptor (TR). Although MSNBs have better pharmacological features than our first generation inhibitors (β-aminoketones), they contain a potentially unstable ester linkage. Here we report the bioisosteric replacement of the ester linkage ...[more]