title: Structure-activity studies of trichothecenes: cytotoxicity of analogues and reaction products derived from T-2 toxin and neosolaniol.
abstract: Forty-two analogues and reaction products derived from T-2 toxin or neosolaniol were assayed for their cytotoxicity to cultured mouse lymphoma cells. Structure-activity relationships confirmed the stereospecific nature of the cytotoxic action of T-2. Cytotoxicity was particularly susceptible to changes at C3, C4, C9, and C10 but was relatively unaffected by changes at C8, which appears to represent a region of steric tolerance in the interaction of T-2 with a cellular constituent. The most potent compounds were T-2, diacetoxyscirpenol, and a series of C8 ester analogues 11 and 31-35.
authors.affiliation: Chemical Defence Establishment, Salisbury, Wiltshire, United Kingdom.
authors.forename: D W
authors.initials: DW
authors.lastname: Anderson
authors.forename: R M
authors.initials: RM
authors.lastname: Black
authors.forename: C G
authors.initials: CG
authors.lastname: Lee
authors.forename: C
authors.initials: C
authors.lastname: Pottage
authors.forename: R L
authors.initials: RL
authors.lastname: Rickard
authors.forename: M S
authors.initials: MS
authors.lastname: Sandford
authors.forename: T D
authors.initials: TD
authors.lastname: Webber
authors.forename: N E
authors.initials: NE
authors.lastname: Williams
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D004354:Drug Screening Assays, Antitumor; D008223:Lymphoma / Q000188:drug therapy; D051379:Mice; D012717:Sesquiterpenes / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D013605:T-2 Toxin; D014255:Trichothecenes / Q000138:chemical synthesis* / Q000627:therapeutic use; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D012717:Sesquiterpenes; D014255:Trichothecenes; C016009:neosolaniol; D013605:T-2 Toxin