1292307-29-9Relevant academic research and scientific papers
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency
Egbertson, Melissa,McGaughey, Georgia B.,Pitzenberger, Steven M.,Stauffer, Shaun R.,Coburn, Craig A.,Stachel, Shawn J.,Yang, Wenjin,Barrow, James C.,Neilson, Lou Anne,McWherter, Melody,Perlow, Debra,Fahr, Bruce,Munshi, Sanjeev,Allison, Timothy J.,Holloway, Katharine,Selnick, Harold G.,Yang, Zhiqiang,Swestock, John,Simon, Adam J.,Sankaranarayanan, Sethu,Colussi, Dennis,Tugusheva, Katherine,Lai, Ming-Tain,Pietrak, Beth,Haugabook, Shari,Jin, Lixia,Chen,Holahan, Marie,Stranieri-Michener, Maria,Cook, Jacquelynn J.,Vacca, Joseph,Graham, Samuel L.
supporting information, p. 4812 - 4819 (2015/10/28)
The IC50 of a beta-secretase (BACE-1) lead compound was improved ～200-fold from 11 μM to 55 nM through the addition of a single methyl group. Computational chemistry, small molecule NMR, and protein crystallography capabilities were used to com
SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
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Page/Page column 214, (2011/05/05)
The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
