Cell-based optimization of novel benzamides as potential antimalarial leads.
Bioorg Med Chem Lett
; 19(24): 6970-4, 2009 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-19879133
ABSTRACT
Screening our in-house compound collection using a cell based Plasmodium falciparum proliferation assay we discovered a known pan-kinase inhibitor scaffold as a hit. Further optimization of this series led us to a novel benzamide scaffold which was devoid of human kinase activity while retaining its antiplasmodial activity. The evolution of this compound series leading to optimized candidates with good cellular potency against multiple strains as well as decent in vivo profile is described in this Letter.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Fosfotransferasas
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Plasmodium falciparum
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Benzamidas
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Inhibidores Enzimáticos
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Antimaláricos
Límite:
Animals
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Humans
Idioma:
En
Año:
2009
Tipo del documento:
Article