Scaffold modification based on Wang's pioneering MDM2–p53 inhibitors led to novel,
chemically stable spiro-oxindole compounds bearing a spiro [3 H-indole-3, 2′-pyrrolidin]-2 …

Despite the achieved progress in developing efficient MDM2-p53 protein-protein interaction
inhibitors (MDM2 inhibitors), the acquired resistance of tumor cells to such p53 activators …

Inhibition of the MDM2–p53 protein–protein interaction is being actively pursued as a new
anticancer therapeutic strategy, and spiro-oxindoles have been designed as a class of …

The p53 pathway is inactivated in almost all types of cancer by mutations in the p53
encoding gene or overexpression of the p53 negative regulators, Mdm2 and/or Mdmx …

Small-molecule inhibitors that block the MDM2-p53 protein–protein interaction (MDM2
inhibitors) are being intensely pursued as a new therapeutic strategy for cancer treatment …

The protein–protein interaction of p53 and MDM2/X is a promising non genotoxic anticancer
target. A rapid and efficient methodology was developed to synthesize the 2, 3′-bis (1′ H …

Screening identified 2-(3-((4, 6-dioxo-2-thioxotetrahydropyrimidin-5 (2H)-ylidene) methyl)-2,
5-dimethyl-1H-pyrrol-1-yl)-4, 5, 6, 7-tetrahydrobenzo [b] thiophene-3-carbonitrile as an …

We previously reported the discovery of a class of spirooxindoles as potent and selective
small-molecule inhibitors of the MDM2–p53 interaction (MDM2 inhibitors). We report herein …

Continued optimization of the N-substituent in the piperidinone series provided potent
piperidinone–pyridine inhibitors 6, 7, 14, and 15 with improved pharmacokinetic properties …

Recently, cancer research protocols have introduced clinical-stage spirooxindole-based
MDM2 inhibitors. However, several studies reported tumor resistance to the treatment. This …