| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361727 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
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.
Graphical abstractIdentification of novel 2-oxatriazines as highly potent pan PI3K/mTOR dual inhibitors and their investigation as potential back up candidates to the clinical compound PKI-587.Figure optionsDownload full-size imageDownload as PowerPoint slide
