Inhibition of Pin1, the essential cell cycle regulator, is likely to lead to interesting biological activities, and inhibitors of Pin1 may serve as anti-cancer drugs. A twisted amide mechanism was proposed based on the mechanistic study on CyP and FKBP. The reduced amide peptide analogues 1 and 2 for Pin1 and CyP respectively were designed based on the likely "twisted amide" isomerization mechanism and synthesized. Both of them were synthesized through 6 steps in 12% yield for the analogue 1, and 27% yield for the analogue 2. The analogue 1 inhibited Pin with the IC50 in a low micromolar and the analogue 2 inhibited CyP with the IC50 in milimolar.