5-Ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-α and mTOR for the treatment of breast cancer

A series of 5-ureidobenzofuran-3-one indoles as potent inhibitors of PI3K-α and mTOR has been developed. In the MDA-MB-361 breast cancer model, the lead compound shrank the tumor size remarkably when dosed at 25 mg/kg iv on days 1, 5, and 9.