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Small-molecule MDM2-p53 inhibitors: recent advances

Lookup NU author(s): Bian Zhang, Emeritus Professor Bernard Golding, Dr Ian HardcastleORCiD



This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License (CC BY-NC-ND).


Potent and selective small-molecule inhibitors of the p53-MDM2 interaction intended for the treatment of p53 wild-type tumors have been designed and optimized in a number of chemical series. This review details recent disclosures of compounds in advanced optimization and features key series that have given rise to clinical trial candidates. The structure–activity relationships for inhibitor classes are discussed with reference to x-ray structures, and common structural features are identified.

Publication metadata

Author(s): Zhang B, Golding BT, Hardcastle IR

Publication type: Review

Publication status: Published

Journal: Future Medicinal Chemistry

Year: 2015

Volume: 7

Issue: 5

Pages: 631-645

Print publication date: 01/04/2015

Acceptance date: 01/01/1900

ISSN (print): 1756-8919

ISSN (electronic): 1756-8927


DOI: 10.4155/fmc.15.13