TABLE 1.
Anti HRV-2 activities of anilinoquinazoline-based kinase inhibitor hitsa
| Compound | Structure | EC50 (µM) |
|---|---|---|
| AZ5385 |
|
0.5 |
| AZ4514 |
|
4.4 |
| AZ4516 |
|
3 |
| AZ6252 |
|
1.5 |
| AZ2538 |
|
1.5 |
| AZ5756 |
|
1.5 |
| AZ5765 |
|
1.5 |
| AZ6610 |
|
1.5 |
| AZ6636 |
|
1.5 |
| AZ8146 |
|
4.4 |
| AZ3426 |
|
5.8 |
| AZ5719 |
|
4.4 |
| Tyrphostin AG1478 |
|
>4b |
| Gefitinib |
|
>4b |
Specific hits, identified by screening of the kinase inhibitor library against HRV-2, were tested for anti-HRV-2 activity in a concentration-dependent inhibition of viral cytopathic effect assay in HeLa cells. Three separate determinations were performed, and the EC50 values were calculated according to a Reed and Muench formula. Known EGFR-TKI AG1478 and gefitinib were also included for comparative purposes.
Lack of anti-HRV-2 activity at the highest non-cytotoxic concentration.