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. Author manuscript; available in PMC: 2017 Jun 16.
Published in final edited form as: J Med Chem. 2016 Apr 21;59(10):4511–4525. doi: 10.1021/acs.jmedchem.5b01762

Table 3.

RAD51 D-Loop Inhibitory and RAD51-ssDNA Binding Stimulatory/Inhibitory Activities of 12a–m, 13a–b, 15a–b, and 16a

graphic file with name nihms859674u3.jpg
Cpd R1 R2 D-Loops
ssDNA binding
Max inhibition effect IC50 (μM) Max effect IC50 (μM)
12a 7-OCH3 -OH 13±12% >100 100±18%↓ 35.0±14.0
12b 7-OCH3 -NO2 17±7% >100 105±47%↑ Stim
12c 7-OCH3 -NH2 100±4% 13.2±2.8 29±8%↓ >100
12d 7-OH -OH 97±8% 27.6±4.9 72±11%↓ >100
12e 7-OH -NO2 13±10% >100 92±21%↓ 57.8±3.0
12f 7-OH -NH2 100±3% 8.4±3.4 82±23%↓ 96.9±44.9
12g 7-OH -N(CH3)2 91±8% 9.8±3.5 34±32%↑ Stim
12i 7-F -NH2 95±6% 25.0±5.1 60±18%↓ 81.5±16.6
12j 7-F -N(CH3)2 31±4% >100 57±28%↑ Stim
12l 7,8-diF -NH2 59±4% 34.0±2.9 42±8%↓ >100
12m 7,8-diF -N(CH3)2 19±15% >100 65±22%↓ Stim
13a 7-OCH3 74±5% 38.6±6.2 16±28%↓ >100
13b 7-OH 53±30% 64.9±31.6 87±10%↓ >100
15a graphic file with name nihms859674t7.jpg -NH2 75±7% 46.1±2.8 117±18%↑ Stim
15b graphic file with name nihms859674t8.jpg -NH2 98±5% 20.0±4.1 79±23%↑ Stim
16 graphic file with name nihms859674t9.jpg -NI(CH3)2 38±4% >100 131±28%↑ Stim
a

“↑” Compound stimulates RAD51-ssDNA binding. “↓”Compound inhibits RAD51-ssDNA binding. “Stim” Compound is a stimulator.