Synthesis and cytotoxic activity of novel C7-functionalized spongiane diterpenes.
Based on two lead cytotoxic spongiane diterpenes, a new series of C7-oxygenated derivatives were synthesized and evaluated for their antitumor activity in vitro against the cancer cell lines HeLa and HEp-2. In general, introduction of either hydroxyl or acetoxy groups at C-7 did not improve the resultant cytotoxicity, while the presence of a butyrate ester led to more active compounds (CC(50)=4.0-9.5 microM).
Arnó
Manuel
M
Departamento de Química Orgánica, Universidad de Valencia, E-46100 Burjassot, Valencia, Spain.
Betancur-Galvis
Liliana
L
González
Miguel A
MA
Sierra
Jelver
J
Zaragozá
Ramón J
RJ
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002087:Butyrates / Q000737:chemistry; D045744:Cell Line, Tumor; D004224:Diterpenes / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D002087:Butyrates; D004224:Diterpenes