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

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

  • J Med Chem. 2003 Nov 6;46(23):4822-5. doi: 10.1021/jm034146v.
Arturo Battaglia 1,  Ralph J Bernacki,  Carlo Bertucci,  Ezio Bombardelli,  Samanta Cimitan,  Cristiano Ferlini,  Gabriele Fontana,  Andrea Guerrini,  Antonella Riva
Affiliations

Affiliation

  • 1 Istituto CNR per La Sintesi Organica e Fotoreattività "I.S.O.F.", via Gobetti 101, 40129 Bologna, Italy. battaglia@area.bo.cnr.it
PMID: 14584931 DOI: 10.1021/jm034146v
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.

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