Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors

[Display omitted] Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and exce...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2016-06, Vol.26 (11), p.2735-2738
Main Authors: Tian, Yuan, Ma, Yao, Gibeau, Craig R., Lahue, Brian R., Shipps, Gerald W., Strickland, Corey, Bogen, Stéphane L.
Format: Article
Language:English
Subjects:
Dose-Response Relationship, Drug
hDM2
Humans
Leucine - chemistry
Models, Molecular
Molecular Structure
p53
Piperidines - chemical synthesis
Piperidines - chemistry
Piperidines - pharmacology
Proto-Oncogene Proteins c-mdm2 - antagonists & inhibitors
Proto-Oncogene Proteins c-mdm2 - metabolism
SAR
Structure-Activity Relationship
Tumor Suppressor Protein p53 - antagonists & inhibitors
Tumor Suppressor Protein p53 - metabolism
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Summary:[Display omitted] Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2016.03.078