J. Dimmock, S. A. Patil, D. Leek
Nov 1, 1987
Citations
0
Influential Citations
11
Citations
Quality indicators
Journal
European Journal of Medicinal Chemistry
Abstract
Abstract 2-Dimethylaminomethyl-1-(4-methoxyphenyl)-prop-2-en-1-one hydrochloride ( IIa ) was shown to have potent activity against P388 cells in vitro , whereas in vivo examination of this derivative and related acrylophenone hydrochlorides revealed little activity against P388 lymphocytic leukemia in mice. The preparation of a variety of bis -Mannich bases designed as prodrugs of certain acrylophenones gave rise to various compounds with in vivo activity. Measurement of the half-lives of seven bis -Mannich bases revealed some structural features affecting the rates of deamination. Both IIa and the related bis -Mannich base ( If ) produced 3-dimethylamino-1-(4-methoxyphenyl)-1-propanone under simulated physiological conditions and this process may represent degradation pathways of acrylophenones and bis -Mannich bases in vivo .