Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2014 Aug 14;57(15):6332-41.
doi: 10.1021/jm500627s. Epub 2014 Jul 9.

Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer

Yosup Rew  1 , Daqing Sun
Affiliations
Review

Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer

Yosup Rew et al. J Med Chem. .

Abstract

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 evaluated in human clinical trials for the treatment of cancer. This article provides an overview of its discovery from the de novo design of the piperidinone series to the structure-activity studies leading to the identification of 1. In addition, this article also describes the preclinical pharmacology and pharmacokinetics of 1, along with its drug metabolism and safety assessment.

PubMed Disclaimer

Substances