Anderson DW, Black RM, Lee CG, Pottage C, Rickard RL, Sandford
MS, Webber TD, Williams NE.Structure-activity studies of
trichothecenes: cytotoxicity of analogues and reaction products
derived from T-2 toxin and neosolaniol.
J Med Chem. 1989 Mar;32(3):555-62.
Chemical Defence Establishment, Salisbury, Wiltshire, United
Kingdom.
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.
PMID: 2918501 |
