2. Academic Validation
  3. Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors

Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2644-7. doi: 10.1016/j.bmcl.2010.02.045.
Arie Zask 1,  Jeroen C Verheijen,  David J Richard,  Joshua Kaplan,  Kevin Curran,  Lourdes Toral-Barza,  Judy Lucas,  Irwin Hollander,  Ker Yu
Affiliations

Affiliation

  • 1 Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA. ariez@aol.com
PMID: 20227881 DOI: 10.1016/j.bmcl.2010.02.045
Abstract

Incorporation of bridged morpholines in monocyclic triazine PI3K/mTOR inhibitors gave compounds with increased mTOR selectivity relative to the corresponding morpholine analogs. Compounds with ureidophenyl groups gave highly potent and selective mTOR inhibitors. Potency and selectivity was demonstrated both in vitro and in vivo through biomarker suppression studies. Select compounds exhibited potent inhibition of tumor growth in nude mouse xenograft assays upon PO and IV administration.

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