Table 1. Biological activity of compounds 296-309
|
Compound |
CYP17A1 inhibition IC50, µM) |
Cell growth inhibition (GI50, µM) |
|
|
LNCaP |
PC-3 |
||
|
296 |
0.9 |
11.0 |
14.8 |
|
297 |
13 |
ND |
ND |
|
298 |
NI |
ND |
ND |
|
299 |
NI |
ND |
ND |
|
300 |
NI |
ND |
ND |
|
301 |
110 |
7.9 |
11.2 |
|
302 |
1.5 |
14.1 |
24.3 |
|
303 |
1.1 |
15.9 |
32.1 |
|
304 |
NI |
ND |
ND |
|
305 |
NI |
>50 |
>50 |
|
306 |
NI |
39.0 |
>50 |
|
307 |
NI |
28.0 |
43.5 |
|
308 |
NI |
ND |
ND |
|
309 |
NI |
ND |
ND |
Notes. Did not inhibit, ND – Did not measure.