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  • Title: Design, synthesis and antiproliferative activity of tripentones: a new series of antitubulin agents.
    Author: Lisowski V, Enguehard C, Lancelot J, Caignard D, Lambel S, Leonce S, Pierre A, Atassi G, Renard P, Rault S.
    Journal: Bioorg Med Chem Lett; 2001 Aug 20; 11(16):2205-8. PubMed ID: 11514171.
    Abstract:
    Structure-activity relationship studies of a new series of tripentones (thieno[2,3-b]pyrrolizin-8-ones), led us to prepare several derivatives with antiproliferative activities. The most promising 3-(3-hydroxy-4-methoxyphenyl)thieno[2,3-b]pyrrolizin-8-one 20 (leukemia L1210, IC(50)=15 nM) was shown to be a potent inhibitor of tubulin polymerization.
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