Cytotoxic activity of some natural and synthetic ent-kauranes.
Atractyligenin (1) and several synthetic derivatives were tested and found to be active against tumor cell replication. Compound 1 was readily converted to the 2,15-diketo (3) or 15-keto (4) derivatives, which contain an alpha,beta-unsaturated ketone. Compounds 3 and 4 showed significant cytotoxic activity against all six tested cancer cell lines and were most potent against 1A9 ovarian cancer cells with EC50 values of 0.2 and 0.3 microM, respectively. These two 1-analogues are promising lead compounds for further investigation.
Rosselli
Sergio
S
Dipartimento di Chimica Organica, Università di Palermo, Viale delle Scienze, 90128 Palermo, Italy.
Bruno
Maurizio
M
Maggio
Antonella
A
Bellone
Gabriella
G
Chen
Tzu-Hsuan
TH
Bastow
Kenneth F
KF
Lee
Kuo-Hsiung
KH
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology; D019659:Asteraceae / Q000737:chemistry; D001278:Atractyloside / Q000031:analogs & derivatives* / Q000494:pharmacology; D045786:Diterpenes, Kaurane / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D019686:Lamiaceae / Q000737:chemistry; D015394:Molecular Structure; D010051:Ovarian Neoplasms; D010946:Plants, Medicinal / Q000737:chemistry; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D045786:Diterpenes, Kaurane; C462123:atractyligenine; D001278:Atractyloside