. 2016 May 27;7(8):785–790. doi: 10.1021/acsmedchemlett.6b00186

Table 2. In Vitro Activity of Analogues in the PSA Luciferase Assay in C4-2-PSA-rl Cells.

entry	compd	EC₅₀ (μM)	entry	compd	EC₅₀ (μM)
1	1	7.3 ± 2.5^c	19	10	20.3 ± 11.6^a
2	5a	>25^a	20	11	>25^a
3	5b	14.5 ± 3.2^b	21	12	>25^b
4	5c	>25^a	22	13	16.1 ± 3.3^b
5	5d	>25^a	23	14	12.7 ± 0.8^a
6	5e	12.0 ± 1.6^b	24	15	2.9 ± 1.0^b
7	5f	12.6 ± 7.7^b	25	16	>25^b
8	5g	11.1 ± 5.3^b	26	18a	>25^b
9	5h	>25^a	27	18b	>25^b
10	5i	18.4 ± 9.2^b	28	18c	7.2 ± 2.7^c
11	5j	11.1 ± 3.3^a	29	20a	>25^a
12	5k	3.1 ± 1.1^a	30	20b	>25^c
13	5l	14.7 ± 4.4^a	31	26a	7.7 ± 1.6^b
14	5m	16.6 ± 4.8^b	32	26b	7.9 ± 2.8^a
15	6	10.8 ± 5.7^b	33	enzalutamide	1.1 ± 0.5^e
16	7	13.7 ± 0.8^b	34	27	2.7 ± 1.1^d
17	8	14.4 ± 3.7^b	35	(1S,2R)-27	1.7 + 0.2^a
18	9	>25^a	36	(1R,2S)-27	15.2 ± 3.3^a

Assay repeats. n = 2.

n = 3.

n = 4.

n = 5.

n = 6. For assay description and complete structural information, please see the Supporting Information and Table S1.