Table 12. Sterling biochemical SAR of N-1, C-5 and C-7 substituted 6,8-difluoro analogs.
Compound | R5 | R7 | R1 |
topo II DNA cleavage
EC50 (µg/ml)a,b |
---|---|---|---|---|
103 WIN 57294 |
H | 2.8 | ||
104 | H | -CH2CH3 | 40 | |
105 | H | >181 | ||
106 | -NH2 | 2.4 |
Compound | R5 | R7 | R1 |
topo II DNA cleavage
EC50 (µg/ml)a,b |
---|---|---|---|---|
103 WIN 57294 |
H | 2.8 | ||
104 | H | -CH2CH3 | 40 | |
105 | H | >181 | ||
106 | -NH2 | 2.4 |