Qingjie Ding

TL;DR: The discovery and characterization of a second generation clinical MDM2 inhibitor, RG7388, with superior potency and selectivity is reported, with a significant challenge for the development of small-molecule inhibitors with desirable pharmacological profiles.

TL;DR: RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket ofMDM2, which stabilizes p53 and activates the p 53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.

TL;DR: The 2,4-diamino-5-ketopyrimidines 6 reported here represent a novel class of potent and ATP-competitive inhibitors that selectively target the cyclin-dependent kinase family, and compound 39 demonstrates significant in vivo efficacy in the HCT116 human colorectal tumor xenograft model in nude mice with up to 95% tumor growth inhibition.

TL;DR: In this article, the authors provided compounds of the formula (I) wherein X, Y, R1, R2, R3, R4, R5, R6 and R7 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof.

TL;DR: Two new potent, selective, and orally active p53-MDM2 antagonists are reported, RO5353 and RO2468, as follow-ups with promising potential for clinical development.