Table 1 Results of biological evaluation

1 [25]

H–

n.d.

5.5

2a

Cl–

25.7 ± 3.5

6.2

2b

F–

28.1 ± 3.3

6.1

2c

Br–

− 5.9 ± 1.3

n.d.

2d

H₃C–

12.4 ± 2.4

n.d.

2e

HO–

0.2 ± 2.5

n.d.

3a

H₃CO–

33.2 ± 3.2

12.2

3b

H₅C₂O–

14.5 ± 1.3

n.d.

3c

C₆H₅–CH₂–O–

12.8 ± 4.9

n.d.

3d

2-hydroxyethoxy–

25.6 ± 3.3

20.0

3e

(2,2-dimethyl-1,3-dioxolan-4-yl)methoxy–

− 11.7 ± 0.7

n.d.

3f

2,3-dihydroxypropoxy–

14.7 ± 1.8

n.d.

3g

HO₂C–CH₂–O

31.3 ± 1.1

n.d.

4a

Dimethylamino–

29.9 ± 5.6

5.7

(+)4b

Diethylamino–

73.0 ± 1.2

1.1

(−)4b

Diethylamino–

− 24.4 ± 10.4

n.d.

4c

Pyrrolidino–

33.0 ± 2.4

n.d.

4d

Piperidino–

39.1 ± 1.1

5.0

4e

Morpholino–

20.2 ± 4.8

n.d.

4f

N-[2-(N-Boc-amino)ethyl)]-N-(methyl)amino–

67.1 ± 2.7

2.5

4g

N⁴-Boc-piperazino–

42.1 ± 2.9

3.8

4h

N-(2-dimethylaminoethyl)-N-(methyl)amino–

99.9 ± 0.1

1.2

4i

N-(2-aminoethyl)-N-(methyl)amino-(as hydrochloride)

8.1 ± 3.3

n.d.

4j

Piperazino-(as hydrochloride)

75.7 ± 1.5

1.5

BS

Blasticidin

99.3 ± 0.7

n.d.