Table 1.
Biological activities of 8-hydroxyquinoline derivatives.
| IN- LEDGF/p75 |
MTT Lncap |
IN 3'-P |
IN ST |
Quench | MTT/MT-4 | |||
|---|---|---|---|---|---|---|---|---|
| (IC50, µM)a | CC50 (µM)b | IC50 (µM)c |
IC50 (µM)d |
% Inhib.e | EC50f | CC50g | SIh | |
| QA | 3.6 ± 0.5 | 5 | >20 | >20 | <50 | ND | ND | |
| QB | 4.3 ± 0.2 | 2.5 | >20 | >20 | <50 | ND | ND | |
| QC | 2.4 ± 0.4 | 2 | >20 | >20 | <50 | ND | ND | |
| Q1-1 | 1.4 ± 0.2 | 0.68 ± 0.03 | >20 | >20 | <50 | ND | ND | |
| Q1–2 | 2.0 ± 1 | 0.58 ± 0.02 | >20 | >20 | <50 | ND | ND | |
| Q1–3 | 2.0 ± 1 | 0.58 ± 0.03 | >20 | >20 | <50 | ND | ND | |
| Q1–4 | 2.6 ± 0.5 | >10 | >20 | >20 | <50 | >10 | 10 | |
| Q1–5 | 3.0 ± 1 | 0.74 ± 0.06 | >20 | >20 | <50 | ND | ND | |
| Q1–6 | 3.5 ± 1.6 | 5 ± 0.6 | >20 | >20 | <50 | ND | ND | |
| Q1–7 | 3.9 ± 1.8 | >10 | >20 | >20 | <50 | >42 | 42 | |
| Q1–8 | 4.0 ± 0 | 0.72 ± 0.1 | >20 | >20 | <50 | ND | ND | |
| Q1–9 | 4.0 ± 0 | 3 ± 0.08 | >20 | >20 | <50 | ND | ND | |
| Q1–10 | 4.0 ± 1 | 0.62 ± 0.03 | >20 | >20 | <50 | ND | ND | |
| Q1–11 | 4.0 ± 3 | 0.62 ± 0.03 | >20 | >20 | <50 | ND | ND | |
| Q1–12 | 4.7 ± 3.4 | 2.4 ± 0.1 | >20 | >20 | <50 | ND | ND | |
| Q2-1 | 1.4 ± 0.1 | >10 | >20 | >20 | <50 | >9 | 9 | |
| Q2-2 | 2.0 ± 0.4 | 0.1 ± 0.02 | >20 | >20 | <50 | ND | ND | |
| Q2–3 | 2.1 ± 0.3 | >10 | >20 | >20 | <50 | >9 | 9 | |
| Q2–4 | 2.8 ± 0.9 | >10 | >20 | >20 | <50 | >2 | 2 | |
| Q2–5 | 2.9 ± 0.5 | >10 | >20 | >20 | <50 | >10 | 10 | |
| Q2–6 | 3.0 ± 0.3 | >10 | >20 | >20 | <50 | >13 | 13 | |
| Q2–7 | 3.2 ± 1.3 | 5 ± 0.2 | >20 | >20 | <50 | ND | ND | |
| Q2–8 | 3.3 ± 1.3 | >10 | >20 | >20 | <50 | 15.41 | 36.5±16.5 | 2 |
| Q2–9 | 3.5 ± 1.2 | >10 | >20 | >20 | <50 | >11 | 11 | |
| Q2–10 | 3.7 ± 2.0 | >10 | >20 | >20 | <50 | >9 | 9 | |
| Q2–11 | 4.0 ± 1.3 | >10 | >20 | >20 | <50 | >9 | 9 | |
| Q2–12 | 4.0 ± 1.7 | >10 | >20 | >20 | <50 | >11 | 11 | |
| Q2–13 | 4.6 ± 1.2 | >10 | >20 | >20 | <50 | 17.85 | 33.5±7.5 | 2 |
| Q2–14 | 4.8 ± 0.3 | >10 | >20 | >20 | <50 | >34 | 34 | |
| Q3-1 | 0.4 ± 0.1 | >10 | >20 | >20 | <50 | >9 | 9 | |
| Q3-2 | 0.8 ± 0.6 | >10 | >20 | >20 | <50 | >35 | 35 | |
| Q3-3 | 1.2 ± 0.5 | >10 | >20 | >20 | <50 | >42 | 42 | |
| Q3–4 | 1.5 ± 0.4 | >10 | >20 | >20 | <50 | >9 | 9 | |
| Q3–5 | 1.9 ± 0.4 | >10 | >20 | >20 | <50 | >9 | 9 | |
| Q3–6 | 2.0 ± 0.2 | >10 | >20 | >20 | <50 | >9 | 9 | |
| Q3–7 | 2.1 ± 1.0 | 5 ± 0.8 | >20 | >20 | <50 | ND | ND | |
| Q3–8 | 2.2 ± 0.4 | >10 | >20 | >20 | <50 | ND | ND | |
| Q3–9 | 2.2 ± 0.4 | >10 | >20 | >20 | <50 | >11 | 11 | |
| Q4-1 | 1.7 ± 0.4 | >10 | >20 | >20 | <50 | >2 | 2 | |
| Q5-1 | 3.0 ± 1 | 0.8 ± 0.06 | >20 | >20 | <50 | >2 | 2 | |
| Q5-2 | 3.0 ± 2 | >10 | >20 | >20 | <50 | ND | ND | |
a
Concentration required to inhibit the in vitro protein-protein interaction by 50%.
b
Cytotoxic concentration reducing Lncap cell viability by 50%.
c
Concentration required to inhibit IN 3’-processing catalysis by 50%.
d
Concentration required to inhibit IN strand transfer catalysis by 50%.
e
Percent inhibition exerted by compounds in quench counter-screen when tested at a concentration of 10 µM.
f
Effective concentration required to reduce HIV-1 induced cytopathic effect by 50% in MT-4 cells.
g
Cytotoxic concentration reducing MT-4 cell viability by 50%.
h
Selectivity index: ratio CC50/EC50.