Ontology highlight
ABSTRACT:
SUBMITTER: Van Dort ME
PROVIDER: S-EPMC5554897 | biostudies-literature | 2017 Aug
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20170724 8
The structure-based design of a new single entity, MEK/PI3K bifunctional inhibitor (<b>7</b>, <b>ST-168</b>), which displays improved MEK1 and PI3K isoform inhibition, is described. <b>ST-168</b> demonstrated a 2.2-fold improvement in MEK1 inhibition and a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ isoforms, respectively, as compared to a previous lead compound (<b>4</b>; <b>ST-162</b>) in <i>in vitro</i> enzymatic inhibition assays. <b>ST-168</b> ...[more]