Design and synthesis of a novel class of furan-based molecules as potential 20S proteasome inhibitors

A novel class of furan-based compounds as potential 20S proteasome inhibitors have been designed and synthesized, among which nine compounds are peptide derivatives and six molecules are statine peptidomimetics. The C-terminal furanyl moiety was introduced to target molecules as furan-based amino acids. All the compounds were obtained steadily with moderate to high yield. Compound 12 was a selective moderate potent proteasome peptidomimetic inhibitor. It inhibited HepG2 and HL-60 proliferation effectively.

Graphical abstractA novel class of furan-based compounds as potential 20S proteasome inhibitors have been designed and synthesized, among which nine compounds are peptide derivatives and six molecules are statine peptidomimetics. All the compounds were obtained steadily with moderate to high yield. Compound 12 was a selective moderate potent proteasome peptidomimetic inhibitor (IC50 = 7.85 μM, CT-L activity). It inhibited HepG2 and HL-60 proliferation effectively (IC50 = 34.2 and 37.07 μM, respectively).Figure optionsDownload full-size imageDownload as PowerPoint slide