SYNTHESIS AND CYTOTOXIC EVALUATION OF SOME STYRYL KETONES AND RELATED-COMPOUNDS

A number of 1-aryl-4-methyl-1-penten-3-ones 1 were converted to the co rresponding Mannich bases 2 and analogues 3. Attempts to form the azin es 4 from several members in series 1 led to the isolation of the corr esponding pyrazolines 5 or aryl aldehyde azines 6. Replacement of the isopropyl group of a compound in series 1 by methyl and ethyl function s led to ketones that reacted with hydrazine producing the correspondi ng azines. The Mannich bases displayed greater activity than the precu rsor ketones towards murine P388 and L1210 leukemia cells as well as t o a panel of human tumour cell lines. Certain of the Mannich bases had selective toxicity towards some human tumour cell lines and others to L1210 cells (in contrast to human T lymphocytes). Several drug-resist ant cell lines were shown to be free from cross resistance to a number of the Mannich bases.