title: Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl]acrylic acid amides and their antimalarial activity.
abstract: Water solubility was previously found to be essential for in vivo-antimalarial activity of a novel type of benzophenone-based farnesyltransferase inhibitors. Introduction of a alpha-amino group into the phenylacetic acid substructure provided more soluble compounds with high farnesyltransferase inhibitory activity. The in vitro-antimalarial activity was detrimentally influenced by this structural modification.
authors.affiliation: Department für Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians Universität München, Butenandtstrasse 5-13, 81377 München, Germany.
authors.forename: Katja
authors.initials: K
authors.lastname: Kettler
authors.forename: Jochen
authors.initials: J
authors.lastname: Wiesner
authors.forename: Katrin
authors.initials: K
authors.lastname: Silber
authors.forename: Peter
authors.initials: P
authors.lastname: Haebel
authors.forename: Regina
authors.initials: R
authors.lastname: Ortmann
authors.forename: Isabel
authors.initials: I
authors.lastname: Sattler
authors.forename: Hans-Martin
authors.initials: HM
authors.lastname: Dahse
authors.forename: Hassan
authors.initials: H
authors.lastname: Jomaa
authors.forename: Gerhard
authors.initials: G
authors.lastname: Klebe
authors.forename: Martin
authors.initials: M
authors.lastname: Schlitzer
mesh_terms: D000178:Acrylamides / Q000138:chemical synthesis* / Q000494:pharmacology; D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051231:Farnesyltranstransferase; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D000178:Acrylamides; D000962:Antimalarials; D004791:Enzyme Inhibitors; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase