Ontology highlight
ABSTRACT:
SUBMITTER: Huang C
PROVIDER: S-EPMC6580565 | biostudies-literature | 2019 Jun
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20190523 6
SMYD3 is a histone methyltransferase that regulates gene transcription, and its overexpression is associated with multiple human cancers. A novel class of tetrahydroacridine compounds which inhibit SMYD3 through a covalent mechanism of action is identified. Optimization of these irreversible inhibitors resulted in the discovery of 4-chloroquinolines, a new class of covalent warheads. Tool compound <b>29</b> exhibits high potency by inhibiting SMYD3's enzymatic activity and showing antiproliferat ...[more]