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. Author manuscript; available in PMC: 2011 Jun 24.
Published in final edited form as: J Med Chem. 2010 Jun 24;53(12):4761–4767. doi: 10.1021/jm100425v

Table 1.

Induction of GST and NQOl by dithiolethiones in rat bladder in vivo

Relative enzyme activity in the bladder (treated/control)
Compd R1 R2 X NQOl GST

graphic file with name nihms207910t1.jpg 1 H H S 2.78 ± 0.11* 1.70 ± 0.04*
2 H H O 1.26 ± 0.09 1.01 ± 0.04
3 CH3 H S 1.83 ± 0.12* 1.23 ± 0.06
4 H CH3 S 1.23 ± 0.06 1.08 ± 0.05
5 CH3 SH S 1.29 ± 0.09 1.08 ± 0.14
6 C6H5 SH S 1.11 ± 0.07 1.03 ± 0.05
7 CO2H H S 3.69 ± 0.30* 2.11 ± 0.15*
8 CO2H CH3 S 1.10 ± 0.04 0.99 ± 0.05
9 H CO2H S 1.27 ± 0.10 1.11 ± 0.07
10 H 4-OH-C6H5 S 1.02 ± 0.05 0.95 ± 0.07
11 CO2CH3 H S 5.05 ± 0.35* 2.69 ± 0.20*
12 CO2C2H5 H S 4.82 ± 0.10* 2.76 ± 0.11*
13 CO2CH3 CH3 S 1.24 ± 0.08 1.24 ± 0.08
14 CO2C2H5 NH2 S 2.03 ± 0.23* 1.25 ± 0.10
15 H CO2C2H5 S 1.13 ± 0.09 1.09 ± 0.04

graphic file with name nihms207910t2.jpg 16 H H S 3.14 ± 0.10* 1.68 ± 0.05*
17 H H O 1.24 ± 0.08* 1.11 ± 0.06
18 H CO2CH3 S 4.39 ± 0.31* 2.31 ± 0.15*
19 H CO2C2H5 S 4.47 ± 0.40* 2.29 ± 0.19*
20 CO2C2H5 H S 1.23 ± 0.04* 1.11 ± 0.07
21 H CH3 S 1.91 ± 0.16* 1.30 ± 0.06*
22 CH3 H S 1.81 ± 0.07* 1.31 ± 0.05*

graphic file with name nihms207910t3.jpg 23 n = 2 1.46 ± 0.09* 1.05 ± 0.03
24 n = 3 1.20 ± 0.07 1.14 ± 0.05
25 n = 4 1.08 ± 0.06 1.11 ± 0.05
*

Significantly different from the corresponding control value (P<0.05). Groups of female Sprague-Dawley rats were dosed with vehicle or the test compound by gavage at 7.5 μmol/kg/day for 10 days and sacrificed on the 11th day. Bladders were promptly removed and assayed for enzymatic activities of GST and NQO1. Each value represents the mean ± SEM of results for the 6 animals in each treatment group.