Synthesis and biological evaluation of methoxylated analogs of the newer generation taxoids IDN5109 and IDN5390

  • Bioorg Med Chem Lett. 2005 Dec 1;15(23):5182-6. doi: 10.1016/j.bmcl.2005.08.066.
Luciano Barboni  1 ,  Roberto Ballini ,  Guido Giarlo ,  Giovanni Appendino ,  Gabriele Fontana ,  Ezio Bombardelli
Affiliations
  • 1. Dipartimento di Scienze Chimiche, Università di Camerino, Via S. Agostino 1, 62032 Camerino (MC), Italy. [email protected]
PMID: 16183281 DOI: 10.1016/j.bmcl.2005.08.066
Abstract

Starting from 10-deacetylbaccatin III (7), the 2-debenzoyl-2-m-methoxybenzoyl analogs of the newer generation taxoids IDN5109 (3) and IDN5390 (4) were synthesized. The biological evaluation of these compounds (5 and 6, respectively) showed a general increase of cytotoxicity, as observed in first-generation Anticancer taxanes.