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. Author manuscript; available in PMC: 2011 May 15.
Published in final edited form as: Bioorg Med Chem. 2010 Mar 27;18(10):3551–3558. doi: 10.1016/j.bmc.2010.03.058

Table 1.

DNA affinities and in vitro antiprotozoan activity for thiazole analogs.

graphic file with name nihms192936t1.jpg
Code a b c d DNA affinity
ΔTm(°C)a 		T. b. r.
IC50(nM) b 		P. f.
IC50(nM) b 		cytotox
IC50(µM) c
5a CH CH CH CH 21.1 4 2.0 36.7
5b N CH CH CH 19.2 4 2.5 1.8
5c CH N CH CH 13.9 16 12.5 102.5
5d CH CH CH N 22.9 6 2.4 40.2
5e N CH CH N 18.2 6 1.1 1.4
5f CH N CH N 12.8 38 13 37. 4
5g CH N N CH 10.0 176 24.6 >195.0
IIa 25 3.2 13.8 6.5
IIc 19.3 7.0 6.5 77.9
IIe 25 3 13.8 51.7
I 12.6 2.8 46.4 46.6
a

Increase in thermal melting of poly(dA−dT)n21

b

The T. b. r. (Trypanosoma brucei rhodesiense) strain was STIB900 and the P. f. (Plasmodium falciparum ) strain was K1. The values are the average of duplicate determinations; 10,28

c

Cyctotoxicity was evaluated using cultured L6 rat myoblast cells; 28