Ontology highlight
ABSTRACT:
SUBMITTER: Chen Z
PROVIDER: S-EPMC6071828 | biostudies-literature | 2017 Jun
REPOSITORIES: biostudies-literature
MedChemComm 20170317 6
As a member of the bromodomain and extra terminal domain (BET) protein family, BRD4 is closely related to cancers and other diseases. Small-molecule BRD4 inhibitors have already demonstrated promising potential for the therapy of BRD4-related cancers. In this study, we report the discovery and evaluation of a novel category of BRD4 inhibitors, which share a trimethoxy ring and target the first bromodomain of the human BRD4 protein. The IC<sub>50</sub> value of the most potent compound, DC-BD-03, ...[more]