Table 16. Banyu eukaryotic biochemical and cellular SAR at quinolone N-1, C-5, C-7 and C-8 positions. Etoposide 14 was used as control.
Compound | R7 | R8 | R5 | R1 |
Induction of DNA cleavable complex
(T/C)a |
L1210 cells CC50
(μg/ml) |
---|---|---|---|---|---|---|
115 | F | -NH2 | 17.3 | 0.006 | ||
116 (-)-BO2367 |
F | H | 15.3 | 0.012 | ||
117 | -OCH3 | H | 14.3 | 0.026 | ||
118 | F | H | 10.0 | 0.17 | ||
119 | F | H | 8.6 | 0.30 | ||
120 | H | H | 6.7 | 0.50 | ||
121 | F | H | 6.7 | 1.1 | ||
122 | H | H | 1.8 | 1.7 | ||
123 | F | H | 1.5 | 4.0 | ||
16 8-F-ciprofloxacin |
F | H | 1.4 | 30 |