When this paper was first published there were errors in Tables 1 and 2. The data for the reference compounds staurosporine and paclitaxel were shifted one column to the left in error, and the activity entry given for staurosporine (0.083 micromolar) is incorrect. The correct tables are printed below.
Table 1. Biological activities and physicochemical properties of series 4 and 5.
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|---|---|---|---|---|---|---|---|---|---|---|
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| GI50 (μM)b | Propertiesc | |||||||||
|
|
|
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| R1 | R3 | IC50 (μM)a Mer TK | A549 | KB | KB-vin | DU145 | MV4-11 | Aq Sol (μg/mL) | Log P | |
| 4a |
|
H | 1.08 | 10.1 | 11.1 | 12.6 | 12.4 | 4.91 | 10.4 | >5 |
| 5a |
|
Me | 1.14 | 9.4 | 11.7 | 10.1 | 10.2 | 2.70 | 1.11 | >5 |
| 4b |
|
H | 0.68 | 15.2 | 20.3 | 17.1 | 18.3 | 8.75 | 95.6 | 2.54 |
| 5b |
|
Me | 2.01 | 13.0 | 24.8 | 30.8 | 30.2 | 70.1 | ND | ND |
| 4c |
|
H | 3.43 | 3.53 | 5.33 | 5.09 | 4.08 | 5.88 | 4.36 | >5 |
| 5c |
|
Me | 1.84 | 12.4 | 13.7 | 12.4 | 13.0 | 2.33e | 3.43 | >5 |
| 4d |
|
H | 2.25 | 16.1 | 14.8 | 17.5 | 14.3 | 3.07 | 6.61 | 3.21 |
| 5d |
|
Me | 10.2 | 19.9 | 18.7 | 22.9 | 24.3 | ND | ND | ND |
| 4e |
|
H | 2.06 | 20.1 | 21.0 | 15.3 | 20.1 | ND | ND | ND |
| 5e |
|
Me | >30 | NDd | ND | ND | ND | ND | ND | ND |
| 4f |
|
H | 3.56 | 13.0 | 13.3 | 13.4 | 13.0 | <13.4 | ND | ND |
| 5g |
|
Me | >30 | ND | ND | ND | ND | ND | ND | ND |
| Staurosporinef | 0.00081 | |||||||||
| Paclitaxel (nM)f | 4.9 | 2.6 | 948 | 2.6 | ND | |||||
The concentration that inhibits 50% Mer tyrosine kinase.
The concentration inhibits 50% human tumor cell growth, averaged values determined by at least three independent experiments.
Active compounds with IC50 < 10 μM and GI50 < 20 μM were measured by the methods in Ref. 19.
Not detected.
Tested in human chronic myelogenous leukemia (K526) cells.
Reference compounds as the positive control in related assays.
Table 2. Biological activities and physicochemical properties of series 6 and 7.
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|---|---|---|---|---|---|---|---|---|---|---|
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| GI50b (μM) | Propertyc | |||||||||
|
|
|
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| R1 | R2 | IC50 (μM)a Mer TK | A549 | KB | KB-vin | DU145 | MV4-11 | Aq Sol (μg/mL) | Log P | |
| 4a |
|
OMe | 1.08 | 10.1 | 11.1 | 12.6 | 12.4 | 4.91 | 10.4 | >5 |
| 6a |
|
CN | >30 | >31.3 | >31.3 | >31.3 | >31.3 | NDd | ND | ND |
| 6b |
|
NH2 | 7.27 | 15.9 | 17.4 | 21.7 | 18.7 | 4.42 | ND | ND |
| 6c |
|
F | 4.17 | 12.8 | 13.8 | 12.3 | 9.9 | 5.43 | 1.54 | >5 |
| 6d |
|
OH | 1.24 | 14.8 | 12.1 | 13.6 | 14.3 | 3.00 | 3.10 | 3.95 |
| 6e |
|
COOH | 2.90 | 28.7 | 25.2 | 19.8 | 27.3 | 7.50 | ND | ND |
| 4b |
|
OMe | 0.68 | 15.2 | 20.3 | 17.1 | 18.3 | 8.75 | 95.6 | 2.54 |
| 7a |
|
CN | 1.72 | 3.00 | 23.7 | 4.31 | 18.7 | 2.79 | 7.52 | 2.84 |
| 7b |
|
NH2 | >30 | 17.1 | 19.7 | 18.7 | 20.8 | ND | ND | ND |
| 7c |
|
F | >30 | 19.3 | 17.1 | 24.2 | 20.6 | ND | ND | ND |
| 7d |
|
F | 7.84 | 4.3 | 2.9 | 2.5 | 4.2 | ND | ND | ND |
| 7e |
|
F | >30 | ND | ND | ND | ND | ND | ND | ND |
| 7f |
|
NH2 | >30 | ND | ND | ND | ND | ND | ND | ND |
| Staurosporinee | 0.00081 | |||||||||
| Paclitaxel (nM)e | 4.9 | 2.6 | 948 | 2.6 | ||||||
IC50 is concentration that inhibits 50% Mer tyrosine kinase.
GI50 is concentration that inhibits 50% human tumor cell growth, and the values were averaged values determined by at least three independent experiments.
Active compounds with IC50 < 10 μM and GI50 < 20 μM were measured by the methods in Ref. 19.
Not detected.
Reference compounds as the positive control in related assays.
The publisher apologises that these errors which were not rectified before publication.