Skip to main content
. Author manuscript; available in PMC: 2014 Jul 1.
Published in final edited form as: Bioorg Med Chem Lett. 2013 May 7;23(13):3826–3832. doi: 10.1016/j.bmcl.2013.04.080

Table 2.

Effects of Ring B substitution on transcription and cytotoxicity in transfected PC-3 cellsa

graphic file with name nihms-477658-t0007.jpg

Cmpd
No.		 R2 IC50 SRE.L
(μM)		 % inh SRE.L
(100 μM)		 % inh WST-1
(100 μM)
2 4-Cl 9.8 78 14
12a PhO 1.5 59 1
12b PhCH2 1.6 59 0
12c 2-Pyr-CH2CH2O 2.3 82 5
12d pyrrolidin-1-yl-SO2 5.6 70 0
12e 2-Me-thiazol-4-yl 6.1 73 1
12f Et 8.1 66 0
12g CH2=CH 11 53 1
12h oxazol-5-yl 12 87 9
12i MeS 12 60 0
12j MeO2C 26 63 0
12k MeO 30 51 0
12l −CN 32 77 0
12m morpholin-1-yl-CH2 32 73 0
12n −NO2 66 65 9
12o MeCO 76 73 0
12p pyrrolidin-1-yl-CH2 ND 94 51
12q 2-CO2Me-furan-4-yl ND 39 0
12r CH2=CHCH2O ND 38 0
12s PhCO ND 38 0
12t 4-methyl-1,2,4-triazol-3-yl ND 36 0
12u 2-oxopyrrolidin-1-yl ND 35 0
12v 3-Cl-4-CF3-pyridin-2-yl-O ND 25 0
12w tBuO2C ND 24 0
a

Assays and abbreviations defined in Table 1.