Table 3.

Classes of compounds identified as inhibitors of the hematin polymerization reaction in HTS

Compound classStructureIC50 (μM) in hematin polymerization assayIC50 (μM) against P. falciparum growth in culture% Inhibition ofP. berghei growth in vivoaIC50 (μM) in cytotoxicity assayb
Chloroquine (Ro 01-6014)Embedded Image800.450.0125100NT
Triarylcarbinol (Ro 06-9075)300.971.1698.44.66
Piperazine (Ro 10-3428)<1000.210.27Inactive4.45
Miscellaneous (Ro 14-3955)241.932.7Inactive63.3
Benzophenone (Ro 22-8014)241.321.7888NT
Imide (Ro 20-1120)131616NTNT
Hydrazide (Ro 04-4410)1915.415.4InactiveNT
Indole (Ro 90-2341)1428.528.5NTNT
Isoxazole (Ro 90-0987)1228.528.5NTNT
  • a Mice were treated p.o. with four doses of each test compound at 100 mg/kg of body weight.

  • b With HeLa cells. NT, not tested.