2. Academic Validation
  3. ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines

ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines

  • J Med Chem. 2009 Aug 27;52(16):5013-6. doi: 10.1021/jm900851f.
Arie Zask 1,  Jeroen C Verheijen,  Kevin Curran,  Joshua Kaplan,  David J Richard,  Pawel Nowak,  David J Malwitz,  Natasja Brooijmans,  Joel Bard,  Kristine Svenson,  Judy Lucas,  Lourdes Toral-Barza,  Wei-Guo Zhang,  Irwin Hollander,  James J Gibbons,  Robert T Abraham,  Semiramis Ayral-Kaloustian,  Tarek S Mansour,  Ker Yu
Affiliations

Affiliation

  • 1 Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA. zaska@wyeth.com
PMID: 19645448 DOI: 10.1021/jm900851f
Abstract

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 of mTOR, only partially inhibit one mTOR protein complex. ATP-competitive, global inhibitors of mTOR that have the potential for enhanced Anticancer efficacy are described. Structural features leading to potency and selectivity were identified and refined leading to compounds with in vivo efficacy in tumor xenograft models.

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