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

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

–

–