Table 3.
Assessment of the anti-cancer activity (IC50) of (−)-agelastatins A–F and advanced intermediates against human cell lines after a 48-hour exposure.a
| Cmpd | U-937 (μM) | HeLa (μM) | A549 (μM) | BT549 (μM) | IMR90 (μM) |
|---|---|---|---|---|---|
| (−)-1 | 0.067 ± 0.003 | 0.708 ± 0.090 | 1.05 ± 0.14 | 0.278 ± 0.076 | 1.11 ± 0.35 |
| (−)-2 | 1.06 ± 0.16 | 4.8 ± 1.2 | >10 | 4.8 ± 1.1 | >10 |
| (−)-3 | >10 | >10 | >10 | >10 | >10 |
| (−)-4 | 0.240 ± 0.033 | 1.00 ± 0.20 | 0.92 ± 0.16 | 0.631 ± 0.082 | 2.75 ± 0.60 |
| (−)-5 | 2.56 ± 0.13 | 8.60 ± 0.81 | >10 | 6.9 ± 2.5 | >10 |
| (−)-6 | >10 | >10 | >10 | >10 | >10 |
| (−)-50 | >10 | >10 | >10 | >10 | >10 |
| (−)-51 | >10 | >10 | >10 | >10 | >10 |
| (−)-52 | >10 | >10 | >10 | >10 | >10 |
| (+)-39 | >10 | >10 | >10 | >10 | >10 |
| (+)-44 | >10 | >10 | >10 | >10 | >10 |
| (+)-45 | >10 | >10 | >10 | >10 | >10 |
| (+)-48 | >10 | >10 | >10 | >10 | >10 |
| (+)-53 | >10 | >10 | >10 | >10 | >10 |
a
Cell lines: U-937, lymphoma; HeLa, cervical carcinoma; A549, non-small cell lung carcinoma; BT549, breast carcinoma; IMR90, immortalized lung fibroblasts; 48-hour IC50 values (in μM) as determined by MTS (U-937) and SRB (HeLa, A549, BT549, and IMR90); MTS = 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium); SRB = sulforhodamine B.