title: Novel CADD-based peptidyl vinyl ester derivatives as potential proteasome inhibitors.
abstract: A series of peptidyl vinyl ester derivatives bearing three different P1 substitutions as potential proteasome inhibitors were studied. The target molecules were designed based on CADD (computer aided drug design) protocol and synthesized. Their activities toward proteasome and four human cancer cell lines (including hepatoma cell line (Bel-7402), myeloid leukemic cell line (HL-60), gastric cancer cell line (BGC-823) and nasopharyngeal cancer cell line (KB)) were tested using fluorescence assay. Two compounds showed proteasome inhibitory activities, and four compounds showed weak antiproliferative activities toward HL-60 and BGC-823.
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: Ke
authors.initials: K
authors.lastname: Mou
authors.forename: Bo
authors.initials: B
authors.lastname: Xu
authors.forename: Chao
authors.initials: C
authors.lastname: Ma
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Yang
authors.forename: Xiaomin
authors.initials: X
authors.lastname: Zou
authors.forename: Yang
authors.initials: Y
authors.lastname: Lü
authors.forename: Ping
authors.initials: P
authors.lastname: Xu
mesh_terms: D000818:Animals; D002417:Cattle; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D004952:Esters / Q000737:chemistry*; D005453:Fluorescence; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D061988:Proteasome Inhibitors; D014753:Vinyl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D004952:Esters; D010446:Peptide Fragments; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; D014753:Vinyl Compounds