Ontology highlight
ABSTRACT:
SUBMITTER: Mahalingam P
PROVIDER: S-EPMC4216204 | biostudies-literature | 2014 Jun
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20140604 12
The 4EGI-1 is the prototypic inhibitor of eIF4E/eIF4G interaction, a potent inhibitor of translation initiation in vitro and in vivo and an efficacious anticancer agent in animal models of human cancers. We report on the design, synthesis, and in vitro characterization of a series of rigidified mimetic of this prototypic inhibitor in which the phenyl in the 2-(4-(3,4-dichlorophenyl)thiazol-2-yl) moiety was bridged into a tricyclic system. The bridge consisted one of the following: ethylene, meth ...[more]