1224979-11-6Relevant articles and documents
4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
Tsou, Hwei-Ru,MacEwan, Gloria,Birnberg, Gary,Zhang, Nan,Brooijmans, Natasja,Toral-Barza, Lourdes,Hollander, Irwin,Ayral-Kaloustian, Semiramis,Yu, Ker
supporting information; experimental part, p. 2259 - 2263 (2010/06/15)
A series of 5-ureidobenzofuranones was discovered as potent and selective inhibitors of mTOR with good cellular activity. Molecular modeling studies revealed several hydrogen bond interactions of the ureido group with the enzyme at the ATP-binding site. Furthermore, modeling showed that the ureido group is best situated at C-5 of the benzofuranone. Syntheses of 4-ureido and 5-ureidobenzofuranones are presented.
