357436-78-3Relevant articles and documents
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 (2007/10/03)
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.
Structure-activity relationships of novel anti-malarial agents. Part 3: N-(4-Acylamino-3-benzoylphenyl)-4-propoxycinnamic acid amides
Wiesner, Jochen,Kettler, Katja,Jomaa, Hassan,Schlitzer, Martin
, p. 543 - 545 (2007/10/03)
We have described 5-(4-propoxycinnamoylamino)-2-(4-tolylacetylamino)benzophenone 6e as a novel lead for anti-malarial agents. Anti-malarial activity of these 5-(4-propoxycinnamoylamino)benzophenones proved to be quite sensitive against variations of the a
Synthesis, molecular modeling, and structure - Activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors
Sakowski,B?hm,Sattler,Dahse,Schlitzer
, p. 2886 - 2899 (2007/10/03)
Because of the involvement of farnesylated proteins in oncogenesis, inhibition of the protein-modifying enzyme farnesyltransferase is considered a major emerging strategy in cancer therapy. Here, we describe the structure - activity relationship of a nove