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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 4.

Probing N4-substituents of N2-furfuryl-quinazolines

graphic file with name nihms665548u4.jpg
Compound R1 R2 L. donovani
EC50a (μM)
J774A.1
EC50b (μM)
SI
3 graphic file with name nihms665548t41.jpg graphic file with name nihms665548t42.jpg 2.5 ± 0.4c 17 ± 6c 6.8
28 graphic file with name nihms665548t43.jpg graphic file with name nihms665548t44.jpg >25 ND ND
29 graphic file with name nihms665548t45.jpg graphic file with name nihms665548t46.jpg >25 ND ND
30 graphic file with name nihms665548t47.jpg graphic file with name nihms665548t48.jpg >25 ND ND
31 graphic file with name nihms665548t49.jpg graphic file with name nihms665548t50.jpg 4.0 ± 2.5 5.3 ± 0.8 1.3
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. 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