1309684-94-3Relevant articles and documents
Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy
Zhang, Zhuming,Ding, Qingjie,Liu, Jin-Jun,Zhang, Jing,Jiang, Nan,Chu, Xin-Jie,Bartkovitz, David,Luk, Kin-Chun,Janson, Cheryl,Tovar, Christian,Filipovic, Zoran M.,Higgins, Brian,Glenn, Kelli,Packman, Kathryn,Vassilev, Lyubomir T.,Graves, Bradford
, p. 4001 - 4009 (2014/08/18)
The field of small-molecule inhibitors of protein-protein interactions is rapidly advancing and the specific area of inhibitors of the p53/MDM2 interaction is a prime example. Several groups have published on this topic and multiple compounds are in various stages of clinical development. Building on the strength of the discovery of RG7112, a Nutlin imidazoline-based compound, and RG7388, a pyrrolidine-based compound, we have developed additional scaffolds that provide opportunities for future development. Here, we report the discovery and optimization of a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitors, culminating in RO8994.
SPIROINDOLINONE PYRROLIDINES
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Page/Page column 35, (2011/06/23)
There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.