Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.

@article{Zhang2014DiscoveryOP,
  title={Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.},
  author={Zhuming Zhang and Xin-Jie Chu and Jin-jun Liu and Qingjie Ding and Jing Zhang and David Bartkovitz and Nan Jiang and Prabha Karnachi and Sung-Sau So and Christian Tovar and Zoran M Filipovic and Brian Higgins and Kelli J Glenn and Kathryn Packman and Lyubomir T. Vassilev and Bradford Graves},
  journal={ACS medicinal chemistry letters},
  year={2014},
  volume={5 2},
  pages={124-7}
}
The development of small-molecule MDM2 inhibitors to restore dysfunctional p53 activities represents a novel approach for cancer treatment. In a previous communication, the efforts leading to the identification of a non-imidazoline MDM2 inhibitor, RG7388, was disclosed and revealed the desirable in vitro and in vivo pharmacological properties that this class of pyrrolidine-based inhibitors possesses. Given this richness and the critical need for a wide variety of chemical structures to ensure… CONTINUE READING
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References

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Showing 1-10 of 23 references

Discovery of RG 7388 , a potent and selective p 53 - MDM 2 inhibitor in clinical development

  • K. Ding, Y. Lu, +10 authors S. Wang
  • J . Med . Chem .
  • 2013

Inhibitors of the p 53 / hdm 2 protein - protein interaction - path to the clinic

  • Y. Ma, B. R. Lahue, +13 authors C. R. Gibeau
  • Bioorg . Med . Chem . Lett .
  • 2013

Effect of the MDM 2 antagonist RG 7112 on the P 53 pathway in patients with MDM 2 - amplified , well - differentiated or dedifferentiated liposarcoma : an exploratory proof - of - mechanism study

  • J.-C. Carry, C. Garcia-Echeverria
  • Lancet Oncol .
  • 2012

Substituted Piperidines that Increase p 53 Activity and the Uses Thereof

  • Q. Ding, Z. Zhang, +13 authors B. Graves
  • 2008

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