title: Design and synthesis of a novel class of furan-based molecules as potential 20S proteasome inhibitors.
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.
authors.affiliation: Department of Medicinal Chemistry, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, PR China.
authors.forename: Yiqiu
authors.initials: Y
authors.lastname: Fu
authors.forename: Bo
authors.initials: B
authors.lastname: Xu
authors.forename: Xiaomin
authors.initials: X
authors.lastname: Zou
authors.forename: Chao
authors.initials: C
authors.lastname: Ma
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Yang
authors.forename: Ke
authors.initials: K
authors.lastname: Mou
authors.forename: Gang
authors.initials: G
authors.lastname: Fu
authors.forename: Yang
authors.initials: Y
authors.lastname: Lü
authors.forename: Ping
authors.initials: P
authors.lastname: Xu
mesh_terms: D000596:Amino Acids / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002918:Chymotrypsin / Q000737:chemistry; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008958:Models, Molecular; D061988:Proteasome Inhibitors
chemical_list: D000596:Amino Acids; D000970:Antineoplastic Agents; D005663:Furans; D061988:Proteasome Inhibitors; D002918:Chymotrypsin