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Synthesis and biological evaluation of 2'-methyl taxoids derived from baccatin III and 14beta-OH-baccatin III 1,14-carbonate.

Abstract
A series of 2'-methyl taxoids were synthesized and essayed for growth inhibition experiments conducted in human ovarian cancer cell line A2780wt and its counterparts A2780cis, A2780tax, and A2780adr, resistant to cisplatin, paclitaxel, and doxorubicin, respectively, to test the effect of this substituent on the antitumor activity. Additional experiments were performed on MCF-7 human breast cancer cell line and MCF7-R resistant to doxorubicin. In several cases these taxoids were more active than paclitaxel showing subnanomolar IC(50) values.
AuthorsArturo Battaglia, Ralph J Bernacki, Carlo Bertucci, Ezio Bombardelli, Samanta Cimitan, Cristiano Ferlini, Gabriele Fontana, Andrea Guerrini, Antonella Riva
JournalJournal of medicinal chemistry (J Med Chem) Vol. 46 Issue 23 Pg. 4822-5 (Nov 06 2003) ISSN: 0022-2623 [Print] United States
PMID14584931 (Publication Type: Journal Article)
Chemical References
  • Alkaloids
  • Antineoplastic Agents
  • Taxoids
  • baccatin III
Topics
  • Alkaloids (chemical synthesis, chemistry, pharmacology)
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm
  • Humans
  • Structure-Activity Relationship
  • Taxoids (chemical synthesis, chemistry, pharmacology)

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