Nonenolizable podophyllotoxin derivatives

To block epimerization and the resulting biological deactivation podophyllotoxin compounds, the lactone carbonyl group has been 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-hydro...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 20; no. 5; pp. 635 - 644
Main Authors Gensler, Walter J, Murthy, C. D, Trammell, Marion H
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 01.05.1977
Subjects
Animals
Cell Survival - drug effects
Cells, Cultured
In Vitro Techniques
Mice
Microtubules - drug effects
Neoplasms, Experimental - metabolism
Podophyllotoxin - analogs & derivatives
Podophyllotoxin - chemical synthesis
Podophyllotoxin - pharmacology
Protein Binding - drug effects
Tubulin - metabolism
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Summary:To block epimerization and the resulting biological deactivation podophyllotoxin compounds, the lactone carbonyl group has been 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.
Bibliography:ark:/67375/TPS-WPBPNQC3-7
istex:1F091504624C99DDE0A2596A626864D314C85A18
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00215a004