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Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.

ABSTRACT: 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.

SUBMITTER: Zhang Z

PROVIDER: S-EPMC4027646 | biostudies-literature | 2014 Feb

REPOSITORIES: biostudies-literature

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Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.

Zhang Zhuming Z Chu Xin-Jie XJ Liu Jin-Jun JJ Ding Qingjie Q Zhang Jing J Bartkovitz David D Jiang Nan N Karnachi Prabha P So Sung-Sau SS Tovar Christian C Filipovic Zoran M ZM Higgins Brian B Glenn Kelli K Packman Kathryn K Vassilev Lyubomir L Graves Bradford B

ACS medicinal chemistry letters 20131229 2

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 su ...[more]

PMID: 24900784

Dataset Information

Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.

Publications

Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.

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