Table 2.
Activity of Neopeltolide (1) and Structural Analogs to Inhibit Proliferation of Human Cancer Cells. IC50 values represent the mean ± SEM of three experiments
| analog | MCF-7 cells | P-388 cells | ||
|---|---|---|---|---|
| efficacy (at 10 mM) | potency (IC50) | efficacy (at 10 mM) | potency (IC50) | |
| neopeltolide (1) | 84% inhibition | 2.2 ± 0.1 nM | 100% inhibition | 0.6 ± 0.2 nM |
| diastereomer 1 (2) | 86% inhibition | 219 ± 59.1 nM | 100% inhibition | 42.3 ± 14.4 nM |
| diastereomer 2 (34) | 88% inhibition | 328 ± 28.4 nM | 100% inhibition | 216 ± 62.3 nM |
| benzoyl ester (44) | 78% inhibition | 5.8 ± 4.7 μM | 75% inhibition | 3.3 ± 2.0 nM |
| octanoyl ester (45) | 33% inhibition | > 10 μM | 25% inhibition | > 10 μM |
| oxazole side chain (4) | nominal inhibition | > 10 μM | 10% inhibition | > 10 μM |
| core pyran-alcohol (43) | nominal inhibition | > 10 μM | nominal inhibition | > 10 μM |
| core pyranone (42) | nominal inhibition | > 10 μM | nominal inhibition | > 10 μM |