Table 2.
RSV inhibitory (EC50) and cytotoxic (CC50) concentrations and selectivity indices (SI) of 1a analogs featuring modifications of section C.a
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Compound No. | Y | R2 | EC50 [µM] | CC50 [µM] | SI |
8a | C=O |
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10 | >90 | >9 |
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8b | C=O |
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1.2 (0.79 to 1.84) | 50 | 42 |
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8c | C=O |
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0.06 (0.04 to 0.1) | 5 | 83 |
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8d | C=O |
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0.14 (0.08 to 0.2) | 1.1 | 8 |
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8e | C=O |
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0.28 (0.21 to undef) | 3.3 | 12 |
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8f | C=O |
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0.41 (0.35 to 0.51) | 30 | 73 |
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8g | C=O |
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0.05 (0.03 to 0.08) | 1.1 | 22 |
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8h | C=O |
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0.21 (0.15 to 0.3) | 30 | 143 |
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8i | C=O |
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0.33 (0.26 to 0.4) | 90 | 273 |
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8j | C=O |
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0.31 (0.16 to 0.6) | 3.3 | 11 |
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8k | C=O |
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0.54 (0.17 to 1.7) | 30 | 56 |
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8l | C=O |
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0.32 (0.26 to 0.4) | 90 | 281 |
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8m | C=O |
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>10 | ND | ND |
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8n | C=O |
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0.06 (0.002 to 1.7) | 30 | 500 |
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8o | C=O |
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1.53 (0.71–3.33) | 16.6 | 11 |
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8p | C=O |
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0.07 (0.06 to 0.09) | 5.5 | 79 |
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8q | CH2 |
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0.5 (0.39 to 0.6) | 10 | 20 |
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8r | SO2 |
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>10 | ND | ND |
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8s | NH |
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>10 | ND | ND |
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8t | NH |
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>10 | ND | ND |
Testing and analysis were carried out as specified for table 1.