Activities of pyrazolo[1,5-a]indole derivatives
| Compound | Inhibition of Topo I | Inhibition of Topo II | MG-MID1-a | |||
|---|---|---|---|---|---|---|
| IC50 | CC | IC50 | CC | by JFCR1-b | by NCI1-c | |
| μM | μM | M | ||||
| GS-1 | 100< | N.T. | 300< | N.T. | −4.12 | N.T. |
| GS-2 | 100< | N.T. | 30 | − | −6.45 | N.T. |
| GS-3 | 100< | N.T. | 20 | − | −4.96 | N.T. |
| GS-4 | 100< | N.T. | 10 | +/− | N.T. | −6.43 |
| GS-5 | ∼10 | − | 20 | − | N.T. | −5.91 |
| CPT | 3 | + | 300< | − | −7.0 | −7.3 |
| VP-16 | 300< | − | 10 | + | −5.2 | −4.9 |
| ICRF-193 | 300< | − | 5 | − | −5.9 | N.T. |
CC, cleavable complex; N.T., not tested; +, involvement of stabilization of relevant topo-DNA cleavable complex; −, no stabilization
↵1-a Mean logarithm of 50% growth-inhibitory concentrations in a human cancer cell line panel.
↵1-b Determined by human cancer cell line panel of Cancer Chemotherapy Center, Japanese Foundation for Cancer Research (39 cell lines).
↵1-c Determined by human cancer cell line panel of National Cancer Institute, National Institutes of Health (47 cell lines).