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. 2017 Mar 10;128:70–78. doi: 10.1016/j.ejmech.2017.01.037

Table 1.

DNA binding, in vitro and in vivo antitrypanosomal activity of the DAPI analogues.

Compound Code ΔTma (°C) Cytotoxb (μM) T. b. rc (nM) SId In vivof(cures)
Image 2 DAPI >27 0.86 18 48 2/4
Image 3 5a 19.2 1.7 3 566 0/4
Image 4 5b >26 15.7 5 3140 3/4
Image 5 5c 15.3 23.5 3 7833 3/4
Image 6 5d >26 29.6 6 4876 4/4
Image 7 5e 22.1 3.2 24 133 4/4
Image 8 5f >26 21.3 4 5325 4/4
Image 9 5g 15.3 2.0 3 666.7 1/4
Image 10 5h 12.1 1.8 5 394 1/4
Image 11 5i 11 7.2 9 800 0/2
Image 12 5j 21.4 2.7 3 900 4/4
Image 13 5k 10 4.5 11 409 0/4
Image 14 8 12.6 29 4869 6 NDe
a

Increase in thermal melting of poly (dA-dT)n.

b

Cytotoxicity was evaluated using cultured L6 rat myoblast cells.

c

The T. b. r. (Trypanosoma brucei rhodesiense) strain was STIB900. The values are the average of duplicate determinations.

d

Selectivity Index for T. b. r. expressed as the ratio: IC50 (L6)/IC50 (T.b.r.).

e

Not determined as in vitro inactive.

f

In vivo efficacy was determined in T. b. rhodesiense (STIB900) infected mice at 4 × 5 mg/kg i.p. dose.