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2-Chloro-, 2-bromo- and 2-azido-1,4,6-androstatriene-3,17-diones were synthesized from 1alpha,2alpha-epoxy-4,6-androstadiene-3,17-dione (2) using HCl, HBr and NaN(3), respectively. Compound 2 was also reacted with NaCN to give 2-cyano-1,4,6-androstatriene-3,17-dione (5) and 2beta-cyano-1alpha-hydroxy-4,6-androstadiene-3,17-dione (6). 6Alpha,7alpha-epoxy-1,4-androstadiene-3,17-dione (8) was reacted with HCl, HBr and NaN(3) to form the corresponding 7beta-chloro-, 7beta-bromo- and 7beta-azido-6alpha-hydroxy-1,4-androstadiene-3,17-diones. The cytotoxic activity of these compounds towards T47D (estrogen-dependent) and MDA-MB231 (estrogen-independent) breast cancer cell lines was evaluated. The 6alpha-hydroxy-7beta-substituted analogs were more active than the 2-substituted analogs on both cell lines. Compound 2 showed the highest selective activity against the T47D (IC(50) 7.1 microM) cell line and 5 showed good cytotoxic activity on MDA-MB231 (IC(50) 18.5 microM) cell line, respectively. The 6alpha,7alpha-epoxy analog 8 also showed high cytotoxic activity on both cell lines (IC(50) 17.3 microM on T47D and IC(50) 26.9 microM on MDA-MB231).
The synthesis and evaluation of 5α-reductase inhibitory activity of some 4-azasteroid-20-ones and 20-oximes and 3β-hydroxy-, 3β-acetoxy-, or epoxy-substituted C₂₁ steroidal 20-ones and 20-oximes having double bonds in the A and/or B ring are described. Inhibitory activity of synthesized compounds was assessed using 5α-reductase enzyme and [1,2,6,7-³H]testosterone as substrate. All synthesized compounds were less active than finasteride (IC₅₀: 1.2 nM). Three 4-azasteroid-2-oximes (compounds 4, 6 and 8) showed good inhibitory activity (IC₅₀: 26, 10 and 11 nM) and were more active than corresponding 4-azasteroid 20-ones (compounds 3, 5 and 7). 3β-Hydroxy-, 3β-acetoxy- and 1α,2α-, 5α,6α- or 6α,7α-epoxysteroid-20-one and -20-oxime derivatives having double bonds in the A and/or B ring showed no inhibition of 5α-reductase enzyme.
A series of epoxy- and/or 20-oxime pregnanes were synthesized from commercially available pregnenolone. Compounds 1, 3, 7, 8 and 11-13 were evaluated for cytotoxicity activity towards LNCaP (androgen-dependent) and PC-3 (androgen-independent) prostate cancer cells. Compound 13 showed the highest activity on both LNCaP (IC(50) 15.17 microM) and PC-3 (IC(50) 11.83 microM) cell lines. Compound 11 showed weak activity on LNCaP cells (IC(50) 71.85 microM) and 8 showed the weak activity on PC-3 cells (IC(50) 68.95 microM), respectively. The 5alpha-reductase II (5AR2) inhibitory effects of compounds 1-3, 5 and 7-13 were investigated in a convenient screening model, in which compounds 5, 8, 11 and 12 were observed to be potential inhibitors of 5alpha-reductase, in particular, the 4-azasteroid 11, that also inhibited cell proliferation of androgen-dependent cells and 8, that in addition inhibited PC-3 cells more potently than LNCaP cells.
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