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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 2.

RAD51 D-Loop Inhibitory and RAD51-ssDNA Binding Stimulatory/Inhibitory Activities of 9a–j and 11a–da

graphic file with name nihms859674u2.jpg
Cpd D-Loops
ssDNA binding
R Max inhibition effect IC50 (μM) Max effect IC50 (μM)
9a 4-N(CH3)2 61 ±4% 27.6±6.0 88±22%↑ Stim
9b 3-NO2 20±8% >100 52±14%↓ >100
9c 3-NH2 79±8% 91.1±10.3 11±9%↓ >100
9d 4-OH 38±3% >100 14±16%↓ >100
9e 4-OCF3 22±8% >100 30±21%↑ Stim
9f 4-NO2 2±21% >100 16±13%↓ >100
9g 4-NH2 100±2% 22.1±2.4 18±11%↓ >100
9h 4-NHEt 91±1% 11.1±1.3 2±24%↑ >100
9i graphic file with name nihms859674t1.jpg 8±7% >100 69±35%↑ Stim
9j graphic file with name nihms859674t2.jpg 68±7% 27.2±3.0 11±19%↓ >100
11a graphic file with name nihms859674t3.jpg 70±13% 71.7±18.1 6±10%↓ >100
11b graphic file with name nihms859674t4.jpg 63±4% 79.4±6.0 7±38%↓ >100
11c graphic file with name nihms859674t5.jpg 5±11% >100 42±17%↑ Stim
11d graphic file with name nihms859674t6.jpg 42±11% >100 56±31%↑ Stim
a

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