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  • Title: Novel C2-C3' N-peptide linked macrocyclic taxoids. Part 1: Synthesis and biological activities of docetaxel analogues with a peptide side chain at C3'.
    Author: Larroque AL, Dubois J, Thoret S, Aubert G, Guénard D, Guéritte F.
    Journal: Bioorg Med Chem Lett; 2005 Nov 01; 15(21):4722-6. PubMed ID: 16165352.
    Abstract:
    A series of novel docetaxel analogues possessing a peptide side chain at the C3'-N position was synthesized. These compounds were designed to mimic a region of the alpha-tubulin loop that is equivalent to the paclitaxel binding pocket in beta-tubulin. Eight new peptidic taxoids were obtained and evaluated as inhibitors of microtubule disassembly, as well as for their cytotoxicity.
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