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Table 1 Cytotoxicity of 15 primaquine derivatives (PQ-TZ 4b to 4p) to human hepatoma cells (HepG2) and monkey kidney cells (BGM), as compared to primaquine

From: Primaquine-thiazolidinones block malaria transmission and development of the liver exoerythrocytic forms

Compound R Cytotoxicity (MDL50 in μM) Toxicity ratios (MDL50) PQ-TZ/PQ
HepG2 BGM HepG2 BGM
4b 2-F NT NT
4c 3-F 1302 ± 1 08 550 ± 43 4.4 2.7
4d 4-F ≥6831 ≥6831 23.3 33.8
4e 2-Cl ≥2193 ≥2193 9.4 10.8
4f 3-Cl 641 ± 31 252 ± 24 2.7 1.2
4g 4-Cl 3984 ± 116 NT 17
4h 2-NO2 1463 ± 1 05 1312 ± 145 6.3 6.5
4i 3-NO2 536 ± 17 523 ± 210 2.3 2.6
4j 4-NO2 ≥6651 ≥6651 28.5 32.9
4k 2-OCH3 ≥6833 ≥6833 29.3 33.8
4l 3-OCH3 ≥6651 ≥6651 28.5 32.9
4m 4-OCH3 ≥6644 ≥6644 28.5 32.9
4n 3-CN ≥2242 ≥2242 9.6 11.0
4o 4-CN ≥6726 ≥6726 28.8 33.3
4p 4-CH3 ≥6651 ≥6651 28.5 32.9
Primaquine   233 ± 5 202 ± 35
  1. Drug concentration that killed 50% of cells using the MTT assay as a readout
  2. NT not tested