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

@article{Zask2009ATPcompetitiveIO,
  title={ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.},
  author={Arie Zask and Jeroen C Verheijen and Kevin J Curran and Joshua Kaplan and David J Richard and Pawel M. Nowak and David J Malwitz and Natasja Brooijmans and Joel Bard and Kristine Svenson and Judy Lucas and Lourdes Toral-Barza and Weiguo Zhang and Irwin Hollander and J. J. Gibbons and Robert T. Abraham and Semiramis Ayral-Kaloustian and Tarek S. Mansour and Ker Yu},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 16},
  pages={5013-6}
}
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… CONTINUE READING

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