AM-8553: a novel MDM2 inhibitor with a promising outlook for potential clinical development.

@article{Bernard2012AM8553AN,
  title={AM-8553: a novel MDM2 inhibitor with a promising outlook for potential clinical development.},
  author={Denzil Bernard and Yujun Zhao and Shaomeng Wang},
  journal={Journal of medicinal chemistry},
  year={2012},
  volume={55 11},
  pages={
          4934-5
        }
}
  • Denzil Bernard, Yujun Zhao, Shaomeng Wang
  • Published in
    Journal of medicinal…
    2012
  • Chemistry, Medicine
  • was determined to be 2.42 μMin a competitive MDM2 binding assay. Changing thestereochemistry of one aryl and the C3 acetic acid substituentin 1 and resolution of the active enantiomer yielded compound2, whose affinity to MDM2 is 50- to 70-fold better than 1.Assisted by computer modeling, the N-alkyl substituent in 2was optimized for its interaction with the Phe19 pocket inMDM2. Substitution at C3 with a methyl group led tostabilization of the desired gauche conformation of thedesigned molecules… CONTINUE READING

    Create an AI-powered research feed to stay up to date with new papers like this posted to ArXiv

    Figures and Topics from this paper.

    Explore Further: Topics Discussed in This Paper

    Citations

    Publications citing this paper.
    SHOWING 1-10 OF 10 CITATIONS

    Targeting Transcription Factors for Cancer Treatment

    VIEW 3 EXCERPTS
    CITES BACKGROUND
    HIGHLY INFLUENCED

    Motif mediated protein-protein interactions as drug targets

    VIEW 2 EXCERPTS
    CITES BACKGROUND

    References

    Publications referenced by this paper.