M. Chu et al., SCH-53823 AND SCH-53825, NOVEL FUNGAL METABOLITES WITH PHOSPHOLIPASE-D INHIBITORY ACTIVITY, Bioorganic & medicinal chemistry letters, 6(5), 1996, pp. 579-584
Two novel phospholipase D (PLD) inhibitors, Sch 53823 (1) and Sch 5382
5 (2), were isolated from a fungal culture. The acetylated derivatives
, Sch 53827 (3) and Sch 53829 (4), were prepared for the purpose of st
ructure determination. The extensive NMR studies of 3 and 4 including
DEFT, COSY, NOESY, HETCOR, and selective INEPT experiments permitted t
he establishment of their structures, as well as relative stereochemis
tries. Among these compounds, 3 exhibited the most potent inhibitory a
ctivity in the phospholipase D assay with the IC50 = 17 mu M.