1000894-87-0Relevant academic research and scientific papers
Core modification of substituted piperidines as Novel inhibitors of HDM2-p53 protein-protein interaction
Pan, Weidong,Lahue, Brian R.,Ma, Yao,Nair, Latha G.,Shipps Jr., Gerald W.,Wang, Yaolin,Doll, Ronald,Bogen, Stéphane L.
, p. 1983 - 1986 (2014/04/17)
The discovery of 3,3-disubstituted piperidine 1 as novel p53-HDM2 inhibitors prompted us to implement subsequent SAR follow up directed towards piperidine core modifications. Conformational restrictions and further functionalization of the piperidine core were investigated as a strategy to gain additional interactions with HDM2. Substitutions at positions 4, 5 and 6 of the piperidine ring were explored. Although some substitutions were tolerated, no significant improvement in potency was observed compared to 1. Incorporation of an allyl side chain at position 2 provided a drastic improvement in binding potency.
Substituted Piperidines that Increase P53 Activity and the Uses Thereof
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Page/Page column 91, (2008/06/13)
In its many embodiments, the present invention discloses novel compounds, as inhibitors of HDM2 protein, methods for preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of treatment, prevention, inhibition, of one or more diseases associated with the HDM2 protein or P53 using such compounds or pharmaceutical compositions.
