900504-98-5Relevant articles and documents
The Synthesis of 5-Amino-dihydrobenzo[b]oxepines and 5-Amino-dihydrobenzo[b]azepines via Ichikawa Rearrangement and Ring-Closing Metathesis
Chwastek, Monika,Pieczykolan, Micha?,Stecko, Sebastian
, p. 9046 - 9074 (2016/10/17)
The combination of Ichikawa's rearrangement and a ring-closing metathesis reaction of allyl carbamates is presented as a method for the preparation of 5-amino-substituted 2,5-dihydro-benzo[b]oxepines, 2,5-dihydro-benzo[b]azepines, and 2,5-dihydro-benzo[b]thiepins. It was demonstrated that the use of nonracemic allyl carbamates enables the synthesis of enantioenriched benzo-fused seven-membered heterocycles. Finally, it was shown that further functionalization of the obtained structures allows access to pharmacologically active 5-amino-substituted 2,3,4,5-tetrahydro-1-benzo[b]oxepine scaffolds.
Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity
Leonard, Kristi,Marugan, Juan Jose,Raboisson, Pierre,Calvo, Raul,Gushue, Joan M.,Koblish, Holly K.,Lattanze, Jennifer,Zhao, Shuyuan,Cummings, Maxwell D.,Player, Mark R.,Maroney, Anna C.,Lu, Tianbao
, p. 3463 - 3468 (2007/10/03)
The disruption of the p53-Hdm2 protein-protein interaction induces cell growth arrest and apoptosis. We have identified the 1,4-benzodiazepine-2,5-dione scaffold as a suitable template for inhibiting this interaction by binding to the Hdm2 protein. Several compounds have been made with improved potency, solubility, and cell-based activities.
