Enol esters as potential prodrugs III. Stability and enzyme-mediated hydrolysis of enol esters of 6′-acetylpapaverin
1982
Abstract Based on results obtained previously from studies of some model α-acyloxystyrenes, 3 enol esters of 6′-acetylpapaverin (6′-AP) were selected for evaluation as potential prodrug forms of the quaternary antitumor agent, coralyne. Their in vitro stability in buffers, plasma and some tissue homogenates was studied. While exhibiting adequate stability in simple aqueous solutions, in biological fluids these enol esters reverted to coralyne apparently as a results of enzymatic catalysis. The results of this study indicate that enol esters of 6′-acetylpapaverin exhibit properties which suggest pharmaceutical utility as prodrugs for enhancing the intracellular levels of coralyne in brain and other tissues.
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