Liu, Qian published the artcileDesign, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors, Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is APN AKT dual inhibitor CD13 kinase antitumor polypharmacol.
Herein a novel series of APN and AKT dual inhibitors were derived from the clin. AKT inhibitor AZD5363. It was demonstrated that most compounds exhibited remarkable APN inhibitory activities with the most potent compound 8b (I) (IC50 = 0.05 ± 0.01 μM) being over 70-fold more potent than the approved APN inhibitor bestatin (IC50 = 3.64 ± 0.56 μM). The moderate AKT inhibitory potencies of target compounds were also confirmed, with 5f (II) and 5h (III) possessing AKT1 IC50 values of 0.12 and 0.27 μM, resp. More importantly, the APN IC50 values of 5f and 5h were 0.96 and 0.21 μM, resp., indicating their balanced APN and AKT dual inhibition. HUVEC tube formation assays confirmed the superior APN inhibitory activities of 5f and 5h relative to bestatin at the cellular level. Western blot anal. demonstrated that 5h could effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT.
ACS Medicinal Chemistry Letters published new progress about Drug design. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Name: tert-Butyl piperidin-4-ylcarbamate.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem