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. Author manuscript; available in PMC: 2017 Nov 1.
Published in final edited form as: Bioorg Med Chem. 2016 Sep 12;24(21):5618–5625. doi: 10.1016/j.bmc.2016.09.028

Table 1. Quinolinequinone activities.

Compounds are as shown in Figure 1, and listed in accordance with their NSC numbers. Percentage RNA binding inhibition values were determined in electrophoretic mobility gel shift assays with 15 µM MA, 15 µM Sell5 RNA ligand, and 100 µM compounds, as shown in Figure 2. Percentage glutathione (GSH) inactivation values were determined by measurement of GSH free sulfhydryl levels after incubation of 200 µM GSH with 200 µM compound for 1 h at 25°C. Percentage MA crosslinking values were determined after 2 h, 25°C incubations of 30 µM MA with 50 µM compound, and measurement of dimer and monomer bands as shown in Figure 5. Fifty percent cytotoxic (CC50) concentrations (in µM) are shown for human embryonic kidney HEK293T (293) cells and for the human T cell lines CEM-SS (CEM) and MT4. Values were determined by MTS assay at 2 d post-treatment with compounds. Values are averages from three (GSH inactivation) or two (all other assays) independent experiments, with standard deviations as shown.

Compound %RNA binding % GSH % MA CC50 values (µM)
inhibition inactivation X-linking 293 CEM MT4
76882 69±26 96±1 47±17 8±6 0.6±0.1 0.7±0.1
76883 36±16 33±12 10±2 22±20 2±0 2±0
76885 22±16 54±23 6±1 7±3 2±0 1±1
76886 28±1 95±0 10±4 8±2 6±0 2±0
76893 26±1 50±9 13±5 9±2 2±1 2±0
81046 21±6 92±3 16±11 9±1 2±0 4±3
81047 99±2 95±3 63±6 17±4 2±1 1±1
81048 50±11 50±4 29±1 18±0 5±0 3±4
81050 39±30 96±2 13±10 5±4 0.7±0.4 1±1
81056 26±13 53±6 11±6 4±3 0.9±0.2 1±1
82130 21±13 3±3 6±1 ND ND ND
84999 76±6 30±4 20±13 7±2 5±0 3±1
102729 73±1 56±1 51±11 18±2 3±0 1±1
105808 31±1 96±1 10±2 4±2 1±0 0.6±0.6
663284 3±3 46±5 8±2 13±5 6±1 2±0