2-(Aminoacylamino)benzophenones: farnesyltransferase inhibition and antimalarial activity

The use of amino acids as acyl substitutents at the 2-amino group of our benzophenone core structure yielded compounds with mainly good to moderate farnesyltransferase inhibitory and moderate antimalarial activity. However, these farnesyltransferase inhibitors display some degree of selectivity towa...

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Published inPharmazie Vol. 60; no. 9; pp. 677 - 682
Main Authors Kettler, K., Wiesner, J., Fucik, K., Sakowski, J., Ortmann, R., Dahse, H.-M., Jomaa, H., Schlitzer, M.
Format Journal Article
LanguageEnglish
Published ESCHBORN Govi-Verlag 01.09.2005
Govi-Verlag Pharmazeutischer Verlag Gmbh
Subjects
Amino Acids - chemistry
Animals
Antimalarials - chemical synthesis
Antimalarials - pharmacology
Benzophenones - chemical synthesis
Benzophenones - pharmacology
Chemistry
Chemistry, Medicinal
Chemistry, Multidisciplinary
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - pharmacology
Erythrocytes - parasitology
Escherichia coli - drug effects
Escherichia coli - enzymology
HeLa Cells
Humans
Life Sciences & Biomedicine
Magnetic Resonance Spectroscopy
Pharmacology & Pharmacy
Physical Sciences
Plasmodium falciparum - drug effects
Plasmodium falciparum - growth & development
Science & Technology
Structure-Activity Relationship
IN-VITRO
AGENTS
ACID
MALARIA PARASITES
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Summary:The use of amino acids as acyl substitutents at the 2-amino group of our benzophenone core structure yielded compounds with mainly good to moderate farnesyltransferase inhibitory and moderate antimalarial activity. However, these farnesyltransferase inhibitors display some degree of selectivity towards malarial parasites since there was no cytotoxic activity observed at 70-80 μM.
Bibliography:0031-7144(20050901)60:9L.677;1-
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ISSN:0031-7144