1026591-19-4Relevant academic research and scientific papers
Non-thiol farnesyltransferase inhibitors: Utilization of the far aryl binding site by arylthienylacryloyl-aminobenzophenones
Mitsch, Andreas,Altenkaemper, Mirko,Sattler, Isabel,Schlitzer, Martin
, p. 9 - 17 (2007/10/03)
We recently described two novel aryl binding sites of farnesyltransferase. The 4- and 5-arylsubstituted thienylacryloyl moieties turned out as appropriate substituents for our benzophenone-based AAX-peptidomimetic capable for occupying the far aryl binding site.
Structure-activity relationships of novel anti-malarial agents part 8. Effect of different central aryls in biarylacryloylaminobenzophenones on antimalarial activity
Wiesner,Mitsch,Altenkaemper,Ortmann,Jomaa,Schlitzer, Martin
, p. 854 - 856 (2007/10/03)
Replacement of the 2,5-disubstituted furyl residue present in the known antimalarial agents 8 by other aryl residues resulted in a more or less reduced antimalarial activity in most cases. The only exemption was the 2,4-thienylene compound 11a displaying activity with an IC50 value of 120 nM. In conclusion, the 2,5-furylene compound 8e remains to represent the most active antimalarial agent in this series of farnesyltransferase inhibitors.
