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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acids / chemistry
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Chemical Phenomena
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Chemistry, Physical
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Chymotrypsin / chemistry
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Drug Design
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Drug Screening Assays, Antitumor
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Furans / chemical synthesis*
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Furans / pharmacology*
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Humans
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Models, Molecular
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Proteasome Inhibitors*
Substances
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Amino Acids
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Antineoplastic Agents
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Furans
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Proteasome Inhibitors
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Chymotrypsin