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This table illustrates that replacements for the methyl of cpd 4 by a variety of alkyl or aryl groups led to total loss of activity showing no toleration for any substituent larger than a methyl group.
| Cpd | R | EC50 Gal4 t |
|---|---|---|
| S11 | Et | >1000 |
| S12 | Bu | >3000 |
| S13 | pent | >3000 |
| S14 | hex | >3000 |
| S15 | iBu | >3000 |
| S16 | cyclopent | >3000 |
| S17 | Ph | >3000 |
