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. 2014 Apr 17;57(10):4134–4153. doi: 10.1021/jm500033r

Table 3. In Vitro Antimalarial Activities of Compounds Tested against P. falciparum Strains.

  W2a (nM)
 D6b (nM)
 TM91C235c (nM)
          
compd IC50 IC90 IC50 IC90 IC50 IC90 RId HEPG2 IC50 (nM) SIe PBMC IC50 (nM) HLM/MLM (min)f
12 11.38 32.50 16.87 34.21 27.74 77.92 2.28/0.95        
13 9.42 18.98 9.72 13.80 14.54 31.85 2.31/1.38 980 104/101/67    
14 23.92   46.52   54.49     2565 107/55/47    
15 56.38   90.97   103.78     2643 47/29/25    
16 6.58 10.70 2.91 5.13 6.71 13.26 2.58/2.08 2729 415/938/407 2814 7/30
17 12.76 18.79 9.30 16.46 11.92 30.27 1.84/1.14 1068 84/115/90   8/60
18 33.78   52.08   56.31     1585 47/30/28    
19 33.85   36.56   40.63     2044 60/56/50    
22 6.47 14.11 3.38 4.56 17.64 36.75 8.06/3.09 1929 299/571/109 52240 6/13
23 6.89 12.10 6.12 10.02 9.19 18.15 1.81/1.21 1111 161/182/121 2607 14/6
24 174.92   211.63   213.74     1230 7/6/6    
25 42.09   47.53   51.60     1281 30/27/25    
20 18.55 38.63 7.47 19.06 22.97 32.90 1.73/2.03 1809 98/242/79    
21 11.77 16.88 6.91 10.47 22.26 47.33 4.52/1.61 1580 134/229/71    
36 15.21 62.21 16.59 31.80 15.21 34.56 1.09/1.96 1922 126/116/126    
37 26.40 35.84 12.75 36.50 28.12 39.85 1.09/0.98 1448 55/114/51    
38 44.58 71.12 19.44 53.02 26.40 45.62 0.86/1.34 5854 131/301/222    
39 34.44 96.36 37.51 74.71 30.29 56.22 0.75/1.29 4463 130/119/147   11/47
40 7.34 12.31 24.12 29.47 27.60 51.93 1.76/0.42 12797 1743/531/464    
42 12.13 16.81 5.35 10.18 6.59 12.59 1.24/1.65 14480 1194/2707/2197   14/47
43 30.47 54.74 31.67 55.88 20.33 28.56 0.51/0.98 2828 93/89/139   11/60
44 8.05 11.69 8.93 10.94 16.34 22.63 2.07/1.07 2360 293/264/144    
50 19.73   42.29   32.42   0.77/0.47g 14096 714/333/435   60/60
51 36.14 81.14 100.81 138.69 88.71 165.04 1.19/0.58 13823 382/137/156 7838  
52 161.44 234.83 143.83 176.12 146.77 220.15 1.25/1.33 5610 35/39/38 7881  
53 194.60 282.49 138.49 233.61 242.74 347.28 1.49/1.21 10419 54/75/43    
54 2.88 3.74 3.60 4.46 6.18 9.20 2.06/0.84 14381 4993/3995/2327 2588 60/60
55 110.05 152.86 112.30 150.03 100.15 128.18 0.85/1.02 4972 45/44/50    
56 1.35 1.35 2.35 2.63 2.90 3.32 1.26/0.51 9212 6824/3920/3176 2516 27/60
57 56.95   151.87   74.58     5278 93/35/71   60/60
60 78.0 105.17 86.77 113.93 85.89 175.28 1.54/0.92 1648 21/19/19    
59 368.93   368.93   368.93     35417 96/96/96    
61 217.77 413.75 244.96 321.27 297.19 312.51 0.97/1.29 2130 10/9/7    
52 98.19   119.64   124.15     3771 38/32/30 302  
63 108.31   143.32   194.74     4678 43/32/24    
9 (CQ) 456.20 697.97 12.27 16.11 138.82 373.25 23.17/43.32        
MFQ 4.93 15.25 15.70 39.09 36.50 134.07 3.43/0.39        
ARTh 6.70 11.50 9.00 12.80 13.40 17.40 1.36/0.90        
a

P. falciparum Indochina W2 clone.

b

P. falciparum African D6 clone.

c

P. falciparum multidrug resistant TM91C235 strain (Thailand).

d

Resistance index (RI) is defined as the ratio of the IC90 for the resistant versus sensitive strain, TM91C235/D6 and W2/D6, respectively.

e

Selectivity index (SI) is defined as ratio of the IC50 for HepG2/W2, HepG2/D6, and HepG2/TM91C235, respectively.

f

Stability of compounds during incubation with human (HLM) and mouse (MLM) liver microsomes.

g

For this compound index is defined as the ratio of the IC50 for the resistant versus sensitive strain, TM91C235/D6 and W2/D6, respectively;

h

Average of greater than eight replicates.