1197165-77-7Relevant articles and documents
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors
Dehnhardt, Christoph M.,Venkatesan, Aranapakam M.,Chen, Zecheng,Delos-Santos, Efren,Ayral-Kaloustian, Semiramis,Brooijmans, Natasja,Yu, Ker,Hollander, Irwin,Feldberg, Larry,Lucas, Judy,Mallon, Robert
, p. 4773 - 4778 (2011/09/16)
We recently described several highly potent, triazine (1) and triazolopyrimidine (2) scaffold-based, dual PI3K/mTOR-inhibitors (e.g., 1, PKI-587) that were efficacious in both in vitro and in vivo models. In order to further optimize these compounds we devised a novel series, the 2-oxatriazines, which also exhibited excellent potency and good metabolic stability. Some 2-oxatriazines showed promising in vivo biomarker suppression and induced apoptosis in the MDA-MB-361 breast cancer xenograft model.