title: Cytotoxic activity of some natural and synthetic ent-kauranes.
abstract: 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.
authors: Dipartimento di Chimica Organica, Università di Palermo, Viale delle Scienze, 90128 Palermo, Italy.
authors: Sergio
authors: S
authors: Rosselli
authors: Maurizio
authors: M
authors: Bruno
authors: Antonella
authors: A
authors: Maggio
authors: Gabriella
authors: G
authors: Bellone
authors: Tzu-Hsuan
authors: TH
authors: Chen
authors: Kenneth F
authors: KF
authors: Bastow
authors: Kuo-Hsiung
authors: KH
authors: Lee
mesh_terms: 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
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D045786:Diterpenes, Kaurane; C462123:atractyligenine; D001278:Atractyloside