Relative binding affinity of novel steroids to androgen receptors in hamster prostate

Figures & data

Figure 1 Steroidal structures.

Figure 2 Reaction sequence for 9, 10a–10e.

Figure 3 Reaction sequence for17a–17d.

Table I.  Relative binding affinity of the novel compounds to the hamster androgen receptor. RBA: Relative binding affinity. CA: Cyproterone acetate. DHT: Dihydrotestosterone.

Compound	IC50 (nM)	% RBA
1 (DHT)	3.2	100
3 (CA)	4.4	72.7
9	4.4	72.7
10a	3.0	100
10b	3.5	91.4
10c	3.2	100
10d	4.0	80.0
10e	4.5	71.1
17a	4.1	78.0
17b	4.3	74.4
17c	3.7	86.5
17d	4.0	80.0

Table II.  Weight of prostate glands ± standard deviations from animals receiving for 6 days different s.c. treatments.Two groups of animals were kept as control, one was injected with 200 μl of sesame oil (Vehicle) and the second with 200 μg of DHT for 6 days (see Experimental Section).

Compound	Prostate Weight (mg)
CONTROL	36.65 ± 2.8
1 (DHT)	88.33 ± 19.7
DHT+9	78.25 ± 12.3
DHT+10a	64.54 ± 7.1
DHT+10b	69.33 ± 8.2
DHT+10c	67.35 ± 9.3
DHT+10d	74.25 ± 6.2
DHT+10e	78.33 ± 6.3
DHT+17a	74.20 ± 9.2
DHT+17b	75.3 ± 12.3
DHT+17c	71.35 ± 10.1
DHT+17d	72.47 ± 14.1