808170-24-3Relevant 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 (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.
Non-thiol farnesyltransferase inhibitors: N-(4-acylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.
Kettler, Katja,Sakowski, Jacek,Silber, Katrin,Sattler, Isabel,Klebe, Gerhard,Schlitzer, Martin
, p. 1521 - 1530 (2007/10/03)
We have designed the nitrophenylfurylacryl-substituted benzophenone 4f as a non-thiol farnesyltransferase inhibitor utilizing a novel aryl binding site of farnesyltransferase. Variation of the 2-acylamino substituent at the benzophenone core structure of
Structure-activity relationships of novel anti-malarial agents. Part 6: N-(4-arylpropionylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides
Wiesner, Jochen,Fucik, Katharina,Kettler, Katja,Sakowski, Jacek,Ortmann, Regina,Jomaa, Hassan,Schlitzer, Martin
, p. 1539 - 1541 (2007/10/03)
We have demonstrated that the p-trifluoromethylphenylpropionylamino residue at the 2-position of the core structure leads to an active benzophenone-type anti-malarial agent. The attempt to improve water solubility by introduction of an amino group into th
