2‐(Arylpropionylamino)‐ and 2‐(Arylacryloylamino)benzophenones: Farnesyltransferase Inhibition and Antimalarial Activity.

Abstract

2005 Furan derivatives R 0060 2-(Arylpropionylamino)-and 2-(Arylacryloylamino)benzophenones: Farnesyltransferase Inhibition and Antimalarial Activity. -Title compounds of type (I) (19 examples) are prepared and tested for their farnesyltransferase inhibition and antimalarial activity. (Ic) shows the greatest antimalarial activity and displays no measurable cytotoxicity in the MTT-assay. Cinnamoyl derivatives [cf. (Id,e)] display fair farnesyltransferase activity but their low solubility prevents any relevant antimalarial activity. -(FUCIK, K.; KETTLER, K.; WIESNER, J.; ORTMANN, R.; UNTERREITMEIER, D.; KRAUSS, J.; BRACHER, F.; JOMAA, H.; SCHLITZER*, M.; Pharmazie 59 (2004) 10, 744-752; Inst. Pharm., Zent. Pharmaforsch.,