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.
Compound | MW (Da) | IC50 (nM) | |||
---|---|---|---|---|---|
Sch10545 Nf2−/− schwannoma cells | Ben-Men-1 NF2−/− meningioma cells | STS26T NF1+/+ MPNST cells | ST8814 NF1−/− MPNST cells | ||
Silvestrol | 654 | 70 | 10 | 10 | 40 |
8b-O-methyl-4’-demethoxy-3’,4’-methylenedioxyrocaglaol | 462 | >2,500 | >2,500 | 5,000 | 10,000 |
Methyl 8b-O-methyl-4’-demethoxy-3’,4’-methylenedioxyrocaglate | 520 | 1,900 | 3,800 | 1,300 | 2,000 |
Rocaglaol | 434 | 60 | 100 | 40 | 90 |
Methyl rocaglate | 492 | 50 | 55 | 25 | 35 |
4’-demethoxy-3’,4’-methylenedioxyrocaglaol | 448 | 65 | 85 | 55 | 120 |
Methyl 4’-demethoxy-3’,4’-methylenedioxyrocaglate | 506 | 60 | 80 | 35 | 70 |
8b-O-methylrocaglaol | 448 | >20,000 | >20,000 | >20,000 | >20,000 |
Didesmethylrocaglamide | 477 | 10 | 5 | 5 | 5 |
Methyl 8b-O-methylrocaglate | 506 | 9,300 | >10,000 | >10,000 | >20,000 |
Rocaglamide | 506 | ND | 15 | 15 | 20 |