Activity of 3 in LNCaP cells. (A) Nuclear uptake of 6 and 8. (B) Cellular cytotoxicity of 3 toward LNCaP
cells after 72 h incubation. (C) RPB1 protein decreases
after treatment with 1 or 3 at 10 μM
for 72 h or doxorubicin (D) at 1 μM for 24 h. (D)
Cellular level of p53 protein increases after treatment 1 or 3 at 10 μM for 72 h or D at 1
μM for 24 h. (E) The p53 responsive genes p21, IGFBP3, and GADD45A are induced
by 3 in a dose-dependent fashion (concentrations are
1, 3, 10 μM) after 72 h treatment. (F) Alkaline comet assay
shows no increase in genomic fragmentation after prolonged incubation
with 3 (48 h, 10 μM). Error bars represents 90%
range; boxes represent the upper and lower quartiles and median.