2. Academic Validation
  3. Synthesis and structure-activity relationships of new second-generation taxoids

Synthesis and structure-activity relationships of new second-generation taxoids

  • Bioorg Med Chem Lett. 1999 Dec 20;9(24):3423-8. doi: 10.1016/s0960-894x(99)00629-0.
I Ojima 1,  T Wang,  M L Miller,  S Lin,  C P Borella,  X Geng,  P Pera,  R J Bernacki
Affiliations

Affiliation

  • 1 Department of Chemistry, State University of New York at Stony Brook, 11794-3400, USA.
PMID: 10617084 DOI: 10.1016/s0960-894x(99)00629-0
Abstract

A series of second-generation taxoids bearing a substituent on the C-2-benzoyl group and modifications at C-3'/C-10 positions was synthesized. These taxoids exhibited 2-3 orders of magnitude higher potency than that of paclitaxel against drug-resistant human breast Cancer cell lines. It is also noteworthy that three taxoids showed almost no difference in activity against drug-resistant and drug-sensitive cell lines, which are categorized as "advanced second generation taxoids".

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