Table 38.
Examples of novel oxalamido derivatives as caspase-3 inhibitors.375
No. |
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Enzyme assays IC50, μM | |
---|---|---|---|
| |||
R | R′ | Casp-3 | |
450 | 4-OCH3 | fluoro | 20.14 |
451 | 4-CH3 | fluoro | 9.67 |
452 | 4-F | fluoro | 3.47 |
453 | 4-OCH3 | 2,3,5,6-tetrafluorophenoxy | >50 |
454 | 4-CH3 | 2,3,5,6-tetrafluorophenoxy | 12.26 |
455 | 4-F | 2,3,5,6-tetrafluorophenoxy | >50 |
456 | 4-Br | 2,3,5,6-tetrafluorophenoxy | >50 |
457 | 4-Cl | 2,3,5,6-tetrafluorophenoxy | >50 |
458 | 4-OCH3 | 2,6-difluorophenoxy | >50 |
459 | 3-OCH3 | 2,6-difluorophenoxy | >50 |
460 | 2-OCH3 | 2,6-difluorophenoxy | 8.4 |
461 | 4-CH3 | 2,6-difluorophenoxy | >50 |
462 | 3-CH3 | 2,6-difluorophenoxy | 25.2 |
463 | 2-CH3 | 2,6-difluorophenoxy | >50 |
464 | 4-F | 2,6-difluorophenoxy | 14.2 |
465 | 2-F | 2,6-difluorophenoxy | >50 |