1144075-49-9Relevant articles and documents
Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K
Verheijen, Jeroen C.,Yu, Ker,Toral-Barza, Lourdes,Hollander, Irwin,Zask, Arie
scheme or table, p. 375 - 379 (2010/04/02)
2-Aryl-4-morpholinothieno[3,2-d]pyrimidines are known PI3K inhibitors. This class of compounds also potently inhibited the homologous enzyme mTOR. Replacement of the morpholine group in these compounds with an 8-oxa-3-azabicyclo[3.2.1]octane group led to mTOR inhibitors with selectivity over PI3K. Optimization of the 2-aryl substituent led to the discovery of 2-(4-ureidophenyl)-thienopyrimidines as highly potent (IC50 1000-fold) over PI3K and good potency in a cellular proliferation assay (IC50 50 nM).