2-(Arylpropionylamino)- and 2-(arylacryloylamino)benzophenones: farnesyltransferase inhibition and antimalarial activity

2005 Furan derivatives R 0060 2-(Arylpropionylamino)- and 2-(Arylacryloylamino)benzophenones: FarnesylInhibition and Antimalarial Activity. — Title compounds of type (I) (19 04- 113 transferase 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., Ludwig-Maximilians-Univ., D-81377 Muenchen, Germany; Eng.) — M. Bohle