Table 1 In vitro antimalarial activity against Plasmodium falciparum K1 strain and cytotoxicity against MRC-5 cells of total synthetic intermediates, 7-hydroxytropolones and methylated derivatives.

From: Antimalarial troponoids, puberulic acid and viticolins; divergent synthesis and structure-activity relationship studies

Compound

IC50 (μM)

Antimalarial activity (K1 strain)

Cytotoxicity (MRC-5)

1 (synthetic)

0.044 ± 0.0029

288.70

23

>56

ND*

24

>50

ND*

25

>47

ND*

26

>47

ND*

27

>50

ND*

28

>50

ND*

29

0.34 ± 0.022

55.85

37

4.33 ± 0.030

0.0034

38

2.09 ± 0.027

0.0013

40

2.12 ± 0.11

102.40

  1. *ND: not determined.
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