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  • Ker Wei Yu, Celine Shi, +17 authors James Joseph Gibbons
  • Medicine
  • Cancer research
  • 2010 (First Published: 15 January 2010)
  • The mammalian target of rapamycin (mTOR) is a major component of the phosphoinositide 3-kinase (PI3K)/AKT signaling pathway that is dysregulated in 50% of all human malignancies. Rapamycin and itsContinue Reading
  • David J. Richard, Jeroen C. Verheijen, Ker Wei Yu, Arie Zask
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 2010 (First Published: 1 April 2010)
  • Potent inhibitors of the mammalian target of rapamycin (mTOR) which contain the triazine scaffold and the (R)-3-methyl morpholine moiety have been identified. Such compounds also demonstrated goodContinue Reading
  • Arie Zask, Jeroen C. Verheijen, +16 authors Ker Wei Yu
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 2009 (First Published: 27 August 2009)
  • The mammalian target of rapamycin (mTOR), a central regulator of growth, survival, and metabolism, is a validated target for cancer therapy. Rapamycin and its analogues, allosteric inhibitors ofContinue Reading
  • Jeroen C. Verheijen, David J. Richard, +13 authors Arie Zask
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 2009 (First Published: 24 December 2009)
  • Design and synthesis of a series of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as potent and selective inhibitors of the mammalian target of rapamycin (mTOR) are described. Optimization of theContinue Reading
  • Arie Zask, Jeroen C. Verheijen, +6 authors Ker Wei Yu
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 2010 (First Published: 1 April 2010)
  • Incorporation of bridged morpholines in monocyclic triazine PI3K/mTOR inhibitors gave compounds with increased mTOR selectivity relative to the corresponding morpholine analogs. Compounds withContinue Reading
  • David J. Richard, Jeroen C. Verheijen, +6 authors Arie Zask
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 2009 (First Published: 1 December 2009)
  • A series of highly potent and selective pyrazolopyrimidine mTOR inhibitors which contain water-solubilizing groups attached to the 6-arylureidophenyl moiety have been prepared. Such derivativesContinue Reading