Potential antineoplastic activity of keto-C-glycosides--a new family of cytostatic agents.
We have examined the biological activity of keto-C-glycosides (KCGs), a new family of drugs displaying antiproliferative and cytotoxic properties on tumor cells. KCG1, the most powerful drug tested on epithelial derived neoplastic cells, was 25-125 times more cytostatic on epithelial cells than on lymphoma. By contrast, KCG10 proved to be more cytostatic on lymphoma than on epithelial cells. Correlations were found between the cytostaticity of KCGs and their lipophilicity, and are discussed within the framework of the structure-activity and the structure-selectivity relationships.
Bennani-Baïti
M I
MI
Laboratoire de Pathologie Cellulaire, Institut de Recherches Scientifiques sur le Cancer (IRSC), CNRS, Villejuif, France.
Lafarge-Frayssinet
C
C
Herscovici
J
J
Monserret
R
R
Antonakis
K
K
Frayssinet
C
C
Uriel
J
J
D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D003510:Cyclohexanes / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006027:Glycosides / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D011714:Pyrans; D011753:Pyrones; D012995:Solubility; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D014867:Water
D000970:Antineoplastic Agents; D003510:Cyclohexanes; D006027:Glycosides; D011714:Pyrans; D011753:Pyrones; D014867:Water; C077806:KCG 1; C077807:KCG 10; D015107:4-Butyrolactone