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

  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},
  volume={5 2},
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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