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. 2021 Jun 29;12(8):1245–1252. doi: 10.1021/acsmedchemlett.1c00032

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
a

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.