3,5-bis(phenylmethylene)-1-(N-arylmaleamoyl)-4-piperidones: a novel group of cytotoxic agents.

摘要: A series of novel 3,5-bis(phenylmethylene)-1-(N-arylmaleamoyl)-4-piperidones 3 have been synthesized which displayed potent cytotoxicity towards human Molt 4/C8 and CEM T-lymphocytes as well murine P388 L1210 leukemic cells. In contrast, the related N-arylmaleamic acids 4 possessed little or no in these four screens. Molecular modeling revealed certain interplanar bond angles interatomic distances were perceived to contribute observed bioactivity providing suggestions for future structural modifications piperidones 3. Evaluation representative compounds on activity N-myristoyltransferase that, at maximum concentration utilized, namely 250 μM, only weak inhibiting properties by some 4. Various members tolerated mice.