Design, synthesis and antiproliferative activity of tripentones: a new series of antitubulin agents |
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| Authors: | Lisowski V Enguehard C Lancelot J Caignard D Lambel S Leonce S Pierre A Atassi G Renard P Rault S |
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| Affiliation: | Centre d'Etudes et de Recherche sur le Médicament de Normandie, UFR des Sciences Pharmaceutiques, 1, rue Vaubénard, 14032 Cedex, Caen, France. |
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| 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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