Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 133, Issue 4, Pages 676-679Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ja108230s
Keywords
-
Categories
Funding
- NIH-NCI [CA127724, CA095441, CA129828]
- NSF [OCI-0503992]
Ask authors/readers for more resources
There is considerable interest in developing non-peptidic, small-molecule alpha-helix mimetics to disrupt alpha-helix-mediated protein protein interactions. Herein, we report the design of a novel pyrrolopyrimidine-based scaffold for such alpha-helix mimetics with increased conformational rigidity. We also developed a facile solid-phase synthetic route that is amenable to divergent synthesis of a large library. Using a fluorescence polarization-based assay, we identified cell-permeable, dual MDMX/MDM2 inhibitors, demonstrating that the designed molecules can act as alpha-helix mimetics.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available