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. Author manuscript; available in PMC: 2016 Aug 15.
Published in final edited form as: Bioorg Med Chem. 2015 Feb 18;23(16):5182–5189. doi: 10.1016/j.bmc.2015.02.020

Table 3.

Probing N2-substituents of N4-methyl-quinazoline-2,4-diamines

graphic file with name nihms665548u3.jpg
Compound R1 R2 L. donovani
EC50a (μM)		 J774A.1
EC50b (μM)		 SI
2 graphic file with name nihms665548t27.jpg graphic file with name nihms665548t28.jpg 0.15 ± 0.02c 15 ± 1c 100
22 graphic file with name nihms665548t29.jpg graphic file with name nihms665548t30.jpg 20 ± 5 ND ND
23 graphic file with name nihms665548t31.jpg graphic file with name nihms665548t32.jpg 4.4 ± 1.2 39 ± 10 8.9
24 graphic file with name nihms665548t33.jpg graphic file with name nihms665548t34.jpg >25 ND ND
25 graphic file with name nihms665548t35.jpg graphic file with name nihms665548t36.jpg >25 ND ND
26 graphic file with name nihms665548t37.jpg graphic file with name nihms665548t38.jpg 7.6 ± 1.3 >133 >17.5
27 graphic file with name nihms665548t39.jpg graphic file with name nihms665548t40.jpg >25 ND ND
a

EC50 value is the mean ± standard deviation of at least three independent experiments. When a mean value could not be ascertained, the reported value is based on at least two determinations. The control drug for the in vitro intracellular antileishmanial assay is amphotericin B, which displays an EC50 = 41 ± 8 nM against L. donovani (n = 20).

b

EC50 value is the mean ± standard deviation of at least three independent experiments. When a mean value could not be ascertained, the reported value is based on two determinations. Podophyllotoxin is the control compound for the in vitro cytotoxicity assay, exhibiting an EC50 = 21 ± 5 nM against the J774.A1 macrophages (n = 11).

c

From Van Horn et al.18