Literature DB >> 11514171

Design, synthesis and antiproliferative activity of tripentones: a new series of antitubulin agents.

V Lisowski1, C Enguehard, J Lancelot, D Caignard, S Lambel, S Leonce, A Pierre, G Atassi, P Renard, S Rault.   

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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Year:  2001        PMID: 11514171     DOI: 10.1016/s0960-894x(01)00403-6

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Sensitization of ovarian carcinoma cells to Bcl-xL-targeting strategies through indirect modulation of Mcl-1 activity by MR22388, a molecule of the tripentone family.

Authors:  Julie Tomasina; Aurélie Malzert-Freon; Florence Giffard; Emilie Brotin; Marie-Hélène Louis; Edwige Abeilard; Sylvain Rault; Pascal Gauduchon; Laurent Poulain
Journal:  J Ovarian Res       Date:  2013-06-05       Impact factor: 4.234

  1 in total

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