Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors. Issue 11 (1st June 2016)

• Record Type: Journal Article
• Authors: Tian, Yuan; Ma, Yao; Gibeau, Craig R.; Lahue, Brian R.; Shipps, Gerald W.; Strickland, Corey; Bogen, Stéphane L.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 11(2016)
• Page Start: 2735
• Page End: 2738
• Publication Date: 2016-06-01
• Subjects: p53 -- hDM2 -- SAR; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.03.078
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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 compound20t with good potencies and excellent CYP450 profiles.