Table 3.
Modifications at C-3.
| |||||||
|---|---|---|---|---|---|---|---|
| Cmpd. | Y | EC50 (nM)a | Solubilityb | Cmpd. | Y | EC50 (nM)a | Solubilityb |
| 11a |
|
474 | 13 ± 1 | 11n |
|
52 | ND |
| 11b |
|
>5000 | <1 | 11o |
|
25 | 55 ± 2 |
| 11c |
|
>5000 | 54 ± 2 | 11p |
|
87 | 55 ± 2 |
| 11d |
|
>5000 | 69 ± 4 | 11q |
|
164 | 60 ± 2 |
| 11e |
|
68 | ND | 11r |
|
152 | 28 ± 1 |
| 11f |
|
40 | <1 | 11s |
|
486 | 54 ± 7 |
| 11g |
|
73 | 15 ± 2 | 11t |
|
10 | 57 ± 5 |
| 11h |
|
150 | 13 ± 1 | 11u |
|
12 | 36 ± 2 |
| 11i |
|
44 | <1 | 11v |
|
58 | 63 ± 1 |
| 11j |
|
126 | ND | 11w |
|
52 | 20 ± 2 |
| 11k |
|
127 | ND | 11x |
|
88 | 53 ± 1 |
| 11l |
|
8 | 4.9 ± 0.5 | 11y |
|
55 | 5 ± 1 |
| 11m |
|
1163 | 19 ± 1 | ||||