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Me
H
O
HO
O
N
CN
H
CF
3
OH
TFA, Et
3
SiH,
CH
2
Cl
2
OH
TFA, Et
3
SiH,
CH
2
Cl
2
X
13
Me
H
Me
H
O
O
HO
HO
O
N
CN
O
N
CN
H
H
CF
3
CF
3
O
OH
14
15
Figure 6.8
Serendipitous discovery of novel tetracyclic AR antagonists.
Table 6.2 Profile of tetracyclic AR antagonists.
Compound
AR Binding Ki (nM)
AR Transactivation IC
50
(nM)
15
10
225
16
23
226
BMS-779333
18
148
BMS-641988
10
56
bicalutamide
38
534
Me
H
O
O
H
4
R
1
6
3
OMe
O
13
N
CN
O
N
CN
12
7
R
2
2
1
O
H
H
H
CF
3
O
O
CF
3
11
9
Me
15, R
1
=OH,R
2
=H
BMS-779333, R
1
=H,R
2
=OH
16
Figure 6.9
Lead compounds for the AR backup program.
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