Design and synthesis of a novel class of furan-based molecules as potential 20S proteasome inhibitors |
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Authors: | Fu Yiqiu Xu Bo Zou Xiaomin Ma Chao Yang Xiaoming Mou Ke Fu Gang Lü Yang Xu Ping |
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Affiliation: | Department of Medicinal Chemistry, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, PR China. |
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Abstract: | 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. |
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