Table 2 Cytotoxicity and selective index (SI) of basic blue 3 and ITT derivatives in vitro
HEK293T | HepG2 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
CC50 (μM)a | SI | CC50 (μM)a | SI | |||||||
3D7 | W2 | MRA-1239 | MRA-1240 | 3D7 | W2 | MRA-1239 | MRA-1240 | |||
basic blue 3 | 0.021 ± 0.0042 | 6.6 | 4.4 | 4.0 | 3.6 | 1.0 ± 0.064 | 312.5 | 208.3 | 192.3 | 169.5 |
ITT-001 | 0.32 ± 0.042 | 28.6 | 28.8 | 9.2 | 8.2 | 4.0 ± 0.85 | 357.1 | 357.1 | 90.1 | 12.6 |
ITT-002 | 0.20 ± 0.021 | 18.7 | 19.2 | 9.7 | 8.2 | > 50 | > 4672.9 | > 4807.7 | > 2415.5 | > 2049.2 |
ITT-003 | 9.2 ± 3.8 | 938.8 | 958.3 | 369.5 | 293.9 | > 50 | > 5102.0 | > 5208.3 | > 2008.0 | > 1597.4 |
ITT-004 | 10.5 ± 3.4 | 929.2 | 853.7 | 397.7 | 344.3 | > 50 | > 4424.8 | > 4065.0 | > 1893.9 | > 1639.3 |
ITT-005 | 0.73 ± 0.093 | 5.3 | 5.0 | 5.6 | 4.0 | 4.6 ± 0.26 | 33.2 | 31.6 | 35.3 | 25.0 |
ITT-006 | 13.6 ± 3.0 | 1283.0 | 850.0 | 494.5 | 462.6 | > 50 | > 3676.5 | > 3125.0 | > 1818.2 | > 1700.7 |
CQ | 2.9 ± 0.27 | 337.2 | 12.9 | 75.2 | 50.0 | 1.8 ± 0.14 | 209.3 | 8.0 | 46.6 | 31.0 |