Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 2, Pages 124-127Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml400359z
Keywords
MDM2; p53; wild-type; small molecule; apoptosis; cancer
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The development of small-molecule MDM2 inhibitors to restore dysfunctional p53 activities represents a novel approach for cancer treatment. In a previous communication, the efforts leading to the identification of a non-imidazoline MDM2 inhibitor, RG7388, was disclosed and revealed the desirable in vitro and in vivo pharmacological properties that this class of pyrrolidine-based inhibitors possesses. Given this richness and the critical need for a wide variety of chemical structures to ensure success in the clinic, research was expanded to evaluate additional derivatives. Here we report two new potent, selective, and orally active p53-MDM2 antagonists, RO5353 and RO2468, as follow-ups with promising potential for clinical development.
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