Bioorganic and Medicinal Chemistry Letters p. 2752 - 2755 (2011)
Update date:2022-08-02
Topics:
Beck, Hilary P.
Degraffenreid, Michael
Fox, Brian
Allen, John G.
Rew, Yosup
Schneider, Stephen
Saiki, Anne Y.
Yu, Dongyin
Oliner, Jonathan D.
Salyers, Kevin
Ye, Qiuping
Olson, Steven
Human murine double minute 2 (MDM2) is a negative regulator of p53, which plays an important role in cell cycle and apoptosis. We report several optimizations to the synthesis of the chromenotriazolopyrimidine series of MDM2-p53 protein-protein interaction inhibitors. Additionally, the in vitro and in vivo stability, pharmacokinetic properties and solubility were improved through N-substitution.
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