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 towards malarial parasites since there was no cytotoxic activity observed at 70-80 microM.
Kettler
K
K
Department für Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians-Universität, München.
Wiesner
J
J
Fucik
K
K
Sakowski
J
J
Ortmann
R
R
Dahse
H M
HM
Jomaa
H
H
Schlitzer
M
M
D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D001577:Benzophenones / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D004912:Erythrocytes / Q000469:parasitology; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development; D013329:Structure-Activity Relationship
D000596:Amino Acids; D000962:Antimalarials; D001577:Benzophenones; D004791:Enzyme Inhibitors