Design of small-molecule inhibitors (MDM2 inhibitors) to block the MDM2–p53 protein–
protein interaction has been pursued as a new cancer therapeutic strategy. In recent years …

As a result of the toxicity of currently available anticancer drugs and the inefficiency of
chemotherapeutic treatments, the design and discovery of effective and selective antitumor …

Structure-based rational design led to the discovery of novel inhibitors of the MDM2–p53
protein–protein interaction. The affinity of these compounds for MDM2 was improved …

We recently reported the discovery of AMG 232 (1), a potent and selective piperidinone
inhibitor of the MDM2-p53 protein–protein interaction. Compound 1 is currently being …

A straightforward and general method has been developed for the synthesis of benzo [4, 5]
imidazo [1, 2-a] pyrimidine and [1, 2, 4] triazolo [1, 5-a] pyrimidine derivatives by simply …

The growth inhibitory activity of p53 tumor suppressor is tightly regulated by interaction with
two negative regulatory proteins, murine double minute 2 (MDM2) and X (MDMX), which are …

We previously reported the discovery of AMG 232, a highly potent and selective
piperidinone inhibitor of the MDM2–p53 interaction. Our continued search for potent and …

Abstract The [1, 2, 4] triazolo [1, 5-a] pyrimidines (TPs) comprise an important class of non-
naturally occurring small molecules that aroused the interest of researches. This scaffold is …

This review presents the last decade of studies on the synthesis of various types of small-
molecule inhibitors of the p53–Mouse double minute 2 homolog (MDM2) protein–protein …

Structural analysis of both the MDM2–p53 protein–protein interaction and several small
molecules bound to MDM2 led to the design and synthesis of tetrasubstituted morpholinone …