Restricted Rotation Analogs of Decarboxylated S-Adenosylmethionine as Inhibitors of Polyamine Biosynthesis.

Abstract The synthesis and preliminary biological evaluation of decarboxylated S-adenosylmethionine analogs 1 and 2 is described. In an L1210 cultured cell assay, these compounds, designed as conformationally restricted active site probes for spermidine and spermine synthase, exhibit LD 50 values of 0.1 and 1.0 mM, respectively. In addition, these compounds have significant effects on levels of cellular polyamines and S-adenosylmethionine.