CAS: 10514-70-2

2,2-Dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one is a potential cancer drug that belongs to the family of bromodomain inhibitors. It inhibits the transcriptional activity of the androgen receptor by binding to its DNA binding domain. This binding prevents the formation of a transcriptionally active complex with other proteins that are required for gene expression. Bromodomain inhibition has been shown to be effective in vivo and in vitro against castration resistant prostate cancer cells. 2,2-Dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one also has an oral bioavailability profile that is suitable for oral administration as a therapeutic agent. This drug also binds to the terminal domain of family members, which may lead to increased potency against these enzymes.

2,2-Dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one