CYTOTOXIC AND ANTICANCER ACTIVITIES OF SOME 1-ARYL-2-DIMETHYTAMINOMETHYL-2-PROPEN-1-ONE HYDROCHLORIDES

A series of 1-aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides demonstrated marked cytotoxicity towards approximately 55 human tumou r cell lines from different neoplastic diseases. In general they were more potent than melphalan and displayed selective toxicity towards hu man leukemic cells. A representative compound, 1-phenyl-2-dimemethyl-a minomethyl-2-propen-1-one hydrochloride (2a), had similar cytoxicity a s melphalan towards murine P388 and L1210 leukemic cells. In addition, 2a reduced the sizes of a number of human tumour xenografts including colon, prostatic and melanotic cancers passaged in athymic mice. Comp ound 2a showed excellent activity towards Ehrlich ascites carcinoma an d B16F1 melanoma in mise which was enhanced using niosomes. One may co nclude from the data generated that 1-aryl-2-dimethylaminomethyl-2-pro pen-1-one hydrochlorides an a novel series of cytotoxic and anticancer agents.