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. Author manuscript; available in PMC: 2015 Feb 1.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Dec 22;24(3):944–948. doi: 10.1016/j.bmcl.2013.12.064

Table 1.

In vitro antitrypanosomal activity against the STIB900 strain of T. brucei rhodesiense and in vitro cytotoxicity against the L6 cell line.

graphic file with name nihms552119t1.jpg
Compd Subst.
pattern
X Y T. b.
rhodesiense
IC50 (nM)
L6
IC50 (nM)
1a 1,4- NHCO CONH 4.7 110,000
2a 1,3- NHCO CONH 51 120,000
3a 1,4- CH2NHCO CONHCH2 9,500 92,000
4a 1,3- CH2NHCO CONHCH2 64,000 >150,000
5a 1,4- CONH CONH 11 50,000
6a 1,3- CONH CONH 120 99,000
7a 1,4- CONH NHCO 120 92,000
8a 1,4- NHCO 4-C6H4CONH 19 >150,000
9a ----- ----- ----- 690 130,000
10a ----- ----- ----- 86 68,000
11 ----- ----- ----- 2.2 19,000
12a ----- CIm ----- 1.5 41,000
13 ----- N ----- 23 89,000
14 ----- CH ----- 2,200 110,000
melarsoprol ----- ----- ----- 3.8 19,000
pentamidineb ----- ----- ----- 1.5 5,100
a

isolated and tested as the dimesylate salt

b

tested as the diisethionate salt