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

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.