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Synthesis and biological evaluation of 4-deacetoxy-1,7-dideoxy azetidine paclitaxel analogues
Qian Cheng1, Hiromasa Kiyota, Marina Yamaguchi
1Laboratory of Applied Bioorganic Chemistry, Division of Life Science, Graduate School of Agricultural Science, Tohoku University, 1-1 Tsutsumidori-Amamiyamachi, Aoba-ku, Sendai 981-8555, Japan.
Bioorganic & Medicinal Chemistry Letters
|March 20, 2003
Abstract:
Three novel 4-deacetoxy-1,7-dideoxy azetidine paclitaxel analogues were synthesized through a convenient route that employed hydroboration-amination and intramolecular S(N)2-type substitution reaction from a natural taxoid taxinine. All analogues have been tested for cytotoxicity against three human tumor cell lines. None of them showed remarkable cytotoxicity compared to paclitaxel against tested tumor cell lines.