TABLE 1
Effect of indenoquinoxaline derivatives on LPS-induced NF-κB/AP-1 transcriptional activity and cytotoxicity in human THP-1Blue monocytic cells
THP-1Blue monocytic cells were treated with the indicated compounds and activated with 200 ng/ml LPS, and secreted alkaline phosphatase reporter activity was monitored.
| Compound | R | IC50 | Compound | R | IC50 | ||
|---|---|---|---|---|---|---|---|
| NF-κB/AP-1 | Toxicity | NF-κB/AP-1 | Toxicity | ||||
| μM | μM | ||||||
| IQ-1S | =N-ONa | 1.8 ± 0.3 | N.T. | IQ-10 |  | 3.6 ± 0.72 | N.T. |
| IQ-2 |  | 0.90 ± 0.21 | N.T. | IQ-11 |  | N.A. | N.T. |
| IQ-3 |  | 1.4 ± 0.42 | N.T. | IQ-12 |  | N.A. | N.T. |
| IQ-4 |  | 0.92 ± 0.33 | N.T. | IQ-13 |  | N.A. | N.T. |
| IQ-5 |  | 6.7 ± 1.4 | N.T. | IQ-14 |  | N.A. | N.T. |
| IQ-6 |  | 4.9 ± 1.1 | N.T. | IQ-15 |  | N.A. | N.T. |
| IQ-7 |  | 3.7 ± 0.72 | N.T. | IQ-16 |  | N.A. | N.T. |
| IQ-8 |  | 2.3 ± 0.54 | N.T. | IQ-17 |  | N.A. | N.T. |
| IQ-9 |  | 3.1 ± 0.60 | N.T. | IQ-18 |  | N.A. | N.T. |
N.A., no inhibition of reporter activity at concentrations <40 μM; N.T., nontoxic at concentrations <40 μM.