Nonenolizable podophyllotoxin derivatives

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Abstract
To block epimerization and the resulting biological deactivation of podophyllotoxin compounds, the lactone carbonyl group was changed to methylene. Syntheses of several of these delactonized derivatives are described, all with modifications in the original lactone ring and some without the 4-hydroxyl group. Several biological assays show that most of the nonenolizable derivatives retain activity. Podophyllotoxin and several of its analogues and derivatives are cytostatic spindle poisons; they have received considerable attention as antitumor agents, some at the clinical level.