. Author manuscript; available in PMC: 2016 Aug 3.

Published in final edited form as: J Med Chem. 2015 Jul 21;58(15):5770–5780. doi: 10.1021/acs.jmedchem.5b00356

Table 1. Efficacy (EC₅₀) and cytotoxicity (IC₅₀) values for diamidine derivatives of pentamidine and heptamidine.

Asterisk indicated that EC₅₀ values are mathematically predicted, but where never reached experimentally due to toxicity. All values reported as +/− standard deviation.

	EC₅₀	IC₅₀	EC₅₀:IC₅₀
Pentamidine	31 ± 2	64 ± 12	0.48
Heptamidine	9 ± 1	15 ± 0.46	0.60
4	14 ± 5.2	30 ± 4.9	0.47
6	75 ± 11	91 ± 8.4	0.82
8	70 ± 12	355 ± 45.1	0.20
9a	40* ± 9.3	13 ± 2.9	3.08
9b	10.5* ± 5.4	11 ± 1.6	0.95
9c	10.4* ± 2.9	5 ± 0.26	2.08
10a	366* ± 14.9	551 ± 35.4	0.66
10b	393* ± 94.2	414 ± 31.2	0.95
10c	256* 68.2	217 ± 16.2	1.18
11	125* 54.4	134 ± 55.8	0.93
12	31 ± 4	210 ± 19.3	0.15
13	30 ±4	N/A	N/A

Table 1. Efficacy (EC50) and cytotoxicity (IC50) values for diamidine derivatives of pentamidine and heptamidine.

Table 1. Efficacy (EC₅₀) and cytotoxicity (IC₅₀) values for diamidine derivatives of pentamidine and heptamidine.