Target fishing reveals PfPYK-1 and PfRab6 as potential targets of an antiplasmodial 4-anilino-2-trichloromethylquinazoline hit compound

[Display omitted] We present investigations about the mechanism of action of a previously reported 4-anilino-2-trichloromethylquinazoline antiplasmodial hit-compound (Hit A), which did not share a common mechanism of action with established commercial antimalarials and presented a stage-specific eff...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2024-03, Vol.102, p.117654-117654, Article 117654
Main Authors: Kieffer, C., Primas, N., Hutter, S., Merckx, A., Reininger, L., Bach, S., Ruchaud, S., Gaillard, F., Laget, M., Amrane, D., Hervé, L., Castera-Ducros, C., Renault, J., Dumètre, A., Rault, S., Doerig, C., Rathelot, P., Vanelle, P., Azas, N., Verhaeghe, P.
Format: Article
Language:English
Subjects:
2-trichloromethylquinazoline
Affinity chromatography
Antimalarials - chemistry
Antiplasmodial hit
Biochemistry, Molecular Biology
Drug-linked matrix
Erythrocytes
Humans
Life Sciences
Malaria, Falciparum - drug therapy
PfPYK-1
PfRab6
Plasmodium falciparum
Structure-Activity Relationship
Target fishing
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Summary:[Display omitted] We present investigations about the mechanism of action of a previously reported 4-anilino-2-trichloromethylquinazoline antiplasmodial hit-compound (Hit A), which did not share a common mechanism of action with established commercial antimalarials and presented a stage-specific effect on the erythrocytic cycle of P. falciparum at 8 
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2024.117654