Table 3. Antiproliferative Activity of 12, 16, 18–20, and 26–29 in the VCaP Prostate Cancer Cell Line Compared with That of 1 and 4a.
compound | 1 | 4 | 12 | 16 | 18 | 19 | 20 | (S)-26 | (S)-27 | (R)-28 | (R)-29 |
---|---|---|---|---|---|---|---|---|---|---|---|
VCaP IC50 (nM) | 149 ± 30 | 92 ± 71 | 2440 ± 2010 | 40 ± 40 | 30 ± 20 | 50 ± 20 | 10 ± 10 | 680 ± 150 | 480 ± 50 | 40 ± 10 | 110 ± 30 |
VCaP cells (WT AR) were cultured in the presence of 30 pM R1881, and the extent of androgen-dependent proliferation was calculated. The VCaP antiproliferative assay was repeated two times or more.