Table 1.

The growth-inhibitory activity of silvestrol and 10 related rocaglates lacking the dioxanyl ring in NF1+/+ STS26T and NF1−/− ST8814 MPNST, Nf2−/− schwannoma, and NF2−/− meningioma cells.

IC50 (nmol/L)
CompoundMW (Da)Sch10545 Nf2−/− schwannoma cellsBen-Men-1 NF2−/− meningioma cellsSTS26T NF1+/+ MPNST cellsST8814 NF1−/− MPNST cells
Silvestrol65470101040
8b-O-methyl-4′-demethoxy-3′,4′-methylenedioxyrocaglaol462>2,500>2,5005,00010,000
Methyl 8b-O-methyl-4′-demethoxy-3′,4′-methylenedioxyrocaglate5201,9003,8001,3002,000
Rocaglaol434601004090
Methyl rocaglate49250552535
4′-demethoxy-3′,4′-methylenedioxyrocaglaol448658555120
Methyl 4′-demethoxy-3′,4′-methylenedioxyrocaglate50660803570
8b-O-methylrocaglaol448>20,000>20,000>20,000>20,000
Didesmethylrocaglamide47710555
Methyl 8b-O-methylrocaglate5069,300>10,000>10,000>20,000
Rocaglamide506ND151520
  • Note: The average IC50 value of each rocaglate was determined by 3-day resazurin proliferation assays as described in Materials and Methods. Didesmethylrocaglamide and rocaglamide were found to possess growth-inhibitory activity similar to or more potent than silvestrol.

  • Abbreviation: ND, not determined.