Table 1.

Biological data on EbS and EbSe derivatives.^a

STRUCTURE	TbHK1% Inhibition (10 µM)	TbHK1 IC50 (µM)	% BSF Growth Inhibition (10 µM)	BSF EC50 (µM)
1b	-	0.05 ± 0.03	-	2.9 ± 0.28
2b	-	2.0 ± 0.5	-	0.03 ± 0.07
6	0.87 ± 7.9%	>10	77.6 ± 4.3%	7.2 ± 0.5
7	12.8 ± 7.6%	>10	98.3 ± 1.3%	0.28 ± 0.1
12	0%	>10	0%	>10
13	0%	>10	0%	>10
19	18.0 ± 0.4%	>10	52.5 ± 4.9%	~10
20	0%	>10	10.9 ± 10.9%	>10
21	2.7 ± 5.1%	>10	55.6 ± 7.5%	~10
22	0%	>10	0%	>10
26	22.8 ± 3.8%	>10	66.5 ± 10.9%	3.8 ± 0.1
27	1.7 ± 0.3%	>10	8.8 ± 22.1%	>10
28	79.0 ± 2.8%	3.16 ± 0.06	38.6 ± 3.8%	13.0 ± 1.5
29	0%	>10	18.0 ± 20.8%	>10
30	0%	>10	0%	>10
31	0%	>10	15.8 ± 47.3%	>10
32	17.2 ± 14.6%	>10	12.0 ± 17.4%	>10
33	18.5 ± 2.8%	>10	0%	>10

^aTrypanosome cultures were assayed in triplicate in a total volume of 40 µL, and the DMSO vehicle was used as a negative control. Percent inhibition was calculated by comparison to the growth of parasites grown with the DMSO controls from each plate. EbS (10 µM) was included in each assay as a positive control. Dose-response curves performed in triplicate for compounds that elicited > 50% growth inhibition at 10 µM were pursued in a 384-well plate format, with 50% effective concentrations (i.e. EC₅₀) determined using GraphPad Prism (version 6.0) software (GraphPad Software, Inc., La Jolla, CA).

^bdata taken from Ref. 5.