Cytotoxic activity of some natural and synthetic guaianolides.
Several natural guaianolides and synthetic derivatives of repin (1) were tested and found to be active against tumor cell replication. Repin (1) and both mono- and di-halohydrin analogues (2, 7-9, 11, 12) showed significant antitumor potency. A more effective compound (17) was obtained by esterificating repin with the paclitaxel side chain.
Bruno
Maurizio
M
Dipartimento di Chimica Organica, Università di Palermo, Viale delle Scienze, 90128 Palermo, Italy. bruno@dicpm.unipa.it
Rosselli
Sergio
S
Maggio
Antonella
A
Raccuglia
Rosa Angela
RA
Bastow
Kenneth F
KF
Lee
Kuo-Hsiung
KH
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D017239:Paclitaxel / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D012717:Sesquiterpenes; C064339:repin; D017239:Paclitaxel