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. Author manuscript; available in PMC: 2013 Apr 15.
Published in final edited form as: Bioorg Med Chem Lett. 2012 Feb 23;22(8):2976–2979. doi: 10.1016/j.bmcl.2012.02.045

Table 2.

Comparisons of IC50s for P. falciparum growth.

graphic file with name nihms360127u2.jpg
compd n R R1 IC50 (nM) Log Da MWb
7a 1 Ph H 519.9 ± 61.2 −1.08 462.5
7b 10 4-PhF H 292.0 ± 53.2 1.67 628.7
7c 10 Bn H 214.6 ± 0.5 2.80 616.8
7d 10 4-PhOMe H 134.2 ± 10.5 4.37 664.8
7e 10 Ph H 113.9 ± 7.6 3.60 574.7
7f 10 C6H11 H 94.4 ± 35.2 3.41 592.9
9a 10 Bn H 1303.5 ± 13.4 5.32 601.8
9b 10 4-PhF H 846.3 ± 0.7 1.66 613.7
9c 10 Ph H 259.2 ± 18.7 4.08 559.7
9d 5 Ph H 156.6 ± 6.5 1.00 489.6
9e 5 Me Me 955.6 ± 2.5 0.21 317.4
9f 1 Ph Me 543.4 ± 79.2 1.89 447.5
9g 10 Me Me 404.2 ± 16.7 1.95 373.5
9h 10 Bn Me 212.0 ± 27.2 6.64 615.8
9i 10 n-Bu Me 155.8 ± 9.0 5.10 513.8
9j 10 2-PhMe Me 143.4 ± 7.0 3.58 615.8
9k 10 Ph Me 143.4 ± 6.3 3.97 573.7
9l 10 C6H11 Me 134.3 ± 1.8 3.64 591.9
9m 10 4-PhOMe Me 130.9 ± 6.6 3.52 663.8
9n 5 Ph Me 48.3 ± 1.5 2.15 503.6
9o 4 Ph Me 18.7 ± 0.3 1.91 489.6
ARTc 7.31 ± 0.14 262.3
ATV 0.28 ± 0.19 366.3
a

measured by 1-octanol–water partition at pH 7.4

b

molecular weights of lipocations 7 and 9 minus the counterion

c

artemisinin