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. 2014 Dec 10;6(2):151–155. doi: 10.1021/ml500408d

Table 2. SAR Studies: Effect of P ↔ N Replacement on Antitrypanosomal Activity and Cytotoxicity.

    T. b. brucei WT EC50 (μM)
 HEK cells CC50 (μM)
cmpd R NR3 PR3a NR3 PR3a
1a C2H5 >100 36.5 ± 3.5 nd >300
1b n–C4H9 2.8 ± 0.2 0.59 ± 0.06b >300 >300b
1c n-C6H13 0.102 ± 0.024 0.037 ± 0.004 21.8 ± 0.3 22.1 ± 1.1
2a C2H5 >100 >100 nd >300
2b n-C4H9 11.5 ± 0.4 0.48 ± 0.11 >300 >300
3b n-C4H9 4.6 ± 0.6 5.9 ± 0.7b >300 >300b
3c n-C6H13 0.023 ± 0.004 0.011 ± 0.004 15.4 ± 0.2 13.4 ± 0.3
a

Data taken from ref (6).

b

EC50 value for R = i-C4H9 (isobutyl).