Cytotoxic and anticancer activities of some 1-aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides

A series of 1-aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides demonstrated marked cytotoxicity towards approximately 55 human tumour cell lines from different neoplastic diseases. In general they were more potent than melphalan and displayed selective toxicity towards human leukemic cells. A representative compound, 1-phenyl-2-dimethyl-aminomethyl-2-propen-1-one hydrochloride (2a), had similar cytotoxicity as 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. Compound 2a showed excellent activity towards Ehrlich ascites carcinoma and B16F1 melanoma in mice which was enhanced using niosomes. One may conclude from the data generated that 1-aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides are a novel series of cytotoxic and anticancer agents.