| abstract |
The present invention designs and synthesizes a series of novel non-covalent small-molecule short peptide proteasome inhibitors, which are dipeptide compounds constructed by a six-membered heterocycle with the structure of general formula (I): Ⅰ The short peptide non-covalent compounds constructed by the six-membered heterocycle of the present invention have good proteasome inhibitory activity, and have a strong in vitro proliferation inhibitory effect on multiple myeloma cell lines such as RPMI8226, H929, and MM-1S. The raw materials required for the synthesis of the compound of the present invention are readily available, the route design is reasonable, the reaction conditions are mild, the yield in each step is high, the operation is simple and convenient, and is suitable for industrial production. |