Table 19. Dainippon SAR at the quinolone 6- and 8-positions suggesting that co-planarity of the 2-thiazole ring is a determent of potency for this scaffold.
Compound | R6 | R8 |
P388 cells
CC50 (μg/ml)a |
---|---|---|---|
130 | CF | N | 0.02 |
145 | N | N | 0.05 |
146 | CF | CH | >10 |
147 | CF | CF | 55 |
aMurine lymphocytic leukemia cell line