Table 1
Chemical structure, physicochemical parameters, and PGP-inhibitory activity of compounds GP05 to GP570
| Compound | R1 | logP | pKa | Ca | EC50Rhodamine 123 | EC50 Daunomycin | |
|---|---|---|---|---|---|---|---|
| Observed | Predicted | ||||||
| GP05 | 3.67 | 8.44 | 5.90 | 1.45 | 0.65 | 1.49 | |
| GP29 | 4.43 | 7.45 | 6.70 | 0.62 | 0.38 | 0.49 | |
| GP31 | 4.93 | 7.33 | 7.24 | 0.26 | 0.14 | 0.26 | |
| GP62 | 3.98 | 7.56 | 7.45 | 0.11 | 0.06 | 0.23 | |
| GP240 | 4.23 | 3.25 | 4.72 | 17.61 | 6.47 | 6.71 | |
| GP339 | 4.05 | 1.70 | 5.87 | 4.57 | 1.54 | 1.43 | |
| GP358 | 5.15 | 1.73 | 4.75 | 17.87 | 8.49 | 6.05 | |
| GP359 | 4.26 | 0.23 | 5.21 | 5.89 | 2.57 | 3.62 | |
| GP360 | 4.60 | −1.46 | 6.48 | 2.57 | 1.65 | 0.58 | |
| GP366 | 4.60 | N.A. | 6.55 | 2.92 | 2.04 | 0.51 | |
| GP388 | 3.87 | 6.67 | 8.07 | 0.36 | 0.13 | 0.06 | |
| GP570 | 3.35 | N.A. | 3.50 | 44.45 | 30.80 | 36.25 | |
General structure of compounds GP05 to GP388
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N.A., not applicable.