title: Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.
abstract: The marine natural product hapalosin and 22 analogs, which incorporated systematic substituent deletions or variations, were prepared. These compounds were evaluated in a cell-based assay for both MDR-reversing activity and general cytotoxicity. Some substituent modifications resulted in lower cytotoxicities, but most structural changes were either detrimental to or did not seriously alter the MDR-reversing activity.
authors.affiliation: Eisai Research Institute, Andover, MA 01810, USA.
authors.forename: C E
authors.initials: CE
authors.lastname: O'Connell
authors.forename: K A
authors.initials: KA
authors.lastname: Salvato
authors.forename: Z
authors.initials: Z
authors.lastname: Meng
authors.forename: B A
authors.initials: BA
authors.lastname: Littlefield
authors.forename: C E
authors.initials: CE
authors.lastname: Schwartz
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000818:Animals; D047630:Depsipeptides; D018432:Drug Resistance, Multiple; D006801:Humans; D020128:Inhibitory Concentration 50; D007769:Lactams / Q000138:chemical synthesis*; D007783:Lactones / Q000138:chemical synthesis*; D051379:Mice; D008956:Models, Chemical; D011994:Recombinant Proteins / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D047630:Depsipeptides; D007769:Lactams; D007783:Lactones; D011994:Recombinant Proteins; C111358:hapalosin