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Antitumor activity of the C-3 derivatized compounds 5a-5k.
| Compd. | C-3 | IC50(μM) |
|
|---|---|---|---|
| K562 | HepG2 | ||
| CPT | 0.07 ± 0.01 | 0.37 ± 0.06 | |
| 2m | = O | 0.03 ± 0.01 | 0.05 ± 0.03 |
| 5a | -OH·H | 0.14 ± 0.09 | 0.70 ± 0.03 |
| 5b | -OH·CH3 | >10 | >10 |
| 5c | -H·H | >10 | >10 |
| 5d | = COOCH2CH3 | 1.24 ± 0.54 | 3.39 ± 0.27 |
| 5e | = COOCH3 | 1.90 ± 0.14 | 4.73 ± 1.24 |
| 5f | -CH2O(CH2)2OCH2- | >10 | >10 |
| 5g | -F·F | >10 | >10 |
| 5h | = NOH | >10 | >10 |
| 5i | = C6H5 | >10 | >10 |
| 5j | = C6H4-4-CF3 | 1.90 ± 0.26 | >10 |
| 5k | = C6H4-4-CH(CH3)2 | >10 | >10 |
