Table 2. SAR of heterotricyclic anilide phthalazinone inhibitors.
Compound | R | (−)-BSA (nM) | (+)-BSA (nM) |
---|---|---|---|
50 | 93 ± 15 | 85 ± 12 | |
51 | >5000 | ND | |
52 | 64 ± 11 | 72 ± 15 | |
53 | 20 ± 5 | 150 ± 20 | |
54 | 4 ± 1 | 30 ± 10 | |
55 | >5000 | ND | |
56 | >5000 | ND | |
57 | >5000 | ND |
All values are average of three independent determinations unless otherwise stated. ND, not determined.