title: Synthesis and biological activity of prodrug inhibitors of the thioredoxin-thioredoxin reductase system.
abstract: A series of palmarumycin prodrugs and water-soluble analogs has been synthesized and assayed for inhibition of the thioredoxin-thioredoxin reductase system. Increased aqueous solubility led to an improved in vivo activity profile.
authors.affiliation: Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA. pwipf@pitt.edu
authors.forename: Peter
authors.initials: P
authors.lastname: Wipf
authors.forename: Stephen M
authors.initials: SM
authors.lastname: Lynch
authors.forename: Garth
authors.initials: G
authors.lastname: Powis
authors.forename: Anne
authors.initials: A
authors.lastname: Birmingham
authors.forename: Erikah E
authors.initials: EE
authors.lastname: Englund
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009281:Naphthalenes / Q000737:chemistry / Q000494:pharmacology; D011355:Prodrugs / Q000138:chemical synthesis* / Q000494:pharmacology; D012995:Solubility; D013141:Spiro Compounds / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013880:Thioredoxin-Disulfide Reductase / Q000037:antagonists & inhibitors*; D013879:Thioredoxins / Q000037:antagonists & inhibitors
chemical_list: D000970:Antineoplastic Agents; D009281:Naphthalenes; D011355:Prodrugs; D013141:Spiro Compounds; C462879:palmarumycin C2; D013879:Thioredoxins; D013880:Thioredoxin-Disulfide Reductase