Steroidal .alpha.-methylene .delta.-lactones as potential antitumor agents

Steroidal .alpha.-methylene .delta.-lactones as potential antitumor agents

Four novel steroidal alpha-methylene delta-lactones have been synthesized and shown to be active against human nasopharyngeal carcinoma (KB) cells in culture. The syntheses involved the use of known alpha-methylenation procedures. In addition, the lactone 6 was directly methylenated by reaction with...

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Veröffentlicht in:Journal of medicinal chemistry 1980-01, Vol.23 (1), p.90-92
Hauptverfasser: Dehal, Shangara S, Marples, Brian A, Stretton, Reginald J, Traynor, John R
Format: Artikel
Sprache:eng
Schlagworte:
Antineoplastic Agents - chemical synthesis
Cell Division - drug effects
Cells, Cultured
Humans
Lactones - chemical synthesis
Lactones - pharmacology
Nasopharyngeal Neoplasms
Structure-Activity Relationship
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Zusammenfassung:Four novel steroidal alpha-methylene delta-lactones have been synthesized and shown to be active against human nasopharyngeal carcinoma (KB) cells in culture. The syntheses involved the use of known alpha-methylenation procedures. In addition, the lactone 6 was directly methylenated by reaction with CH2O/KOH or Et2NH/CH2O/Et2NH.HCl. The formation of a cysteine adduct (15) with the alpha-methylene lactone 10 is reported.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00175a019