Cytotoxic activity of some natural and synthetic guaianolides

  • J Nat Prod. 2005 Jul;68(7):1042-6. doi: 10.1021/np0500575.
Maurizio Bruno  1 ,  Sergio Rosselli ,  Antonella Maggio ,  Rosa Angela Raccuglia ,  Kenneth F Bastow ,  Kuo-Hsiung Lee
Affiliations
  • 1. Dipartimento di Chimica Organica, Università di Palermo, Viale delle Scienze, 90128 Palermo, Italy. [email protected]
PMID: 16038545 DOI: 10.1021/np0500575
Abstract

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.