847147-38-0Relevant academic research and scientific papers
Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3- benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl]acrylic acid amides and their antimalarial activity
Kettler, Katja,Wiesner, Jochen,Silber, Katrin,Haebel, Peter,Ortmann, Regina,Sattler, Isabel,Dahse, Hans-Martin,Jomaa, Hassan,Klebe, Gerhard,Schlitzer, Martin
, p. 93 - 101 (2005)
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 α-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.
