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

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...

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Published in:Bioorganic & medicinal chemistry letters 2001-08, Vol.11 (16), p.2205-2208
Main Authors: Lisowski, Vincent, Enguehard, Cécile, Lancelot, Jean-Charles, Caignard, Daniel-Henri, Lambel, Stéphanie, Leonce, Stéphane, Pierre, Alain, Atassi, Ghanem, Renard, Pierre, Rault, Sylvain
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Drug Screening Assays, Antitumor
General aspects
Humans
Leukemia L1210 - pathology
Medical sciences
Mice
Pharmacology. Drug treatments
Pyrrolizidine Alkaloids - chemical synthesis
Pyrrolizidine Alkaloids - chemistry
Pyrrolizidine Alkaloids - pharmacology
Structure-Activity Relationship
Tubulin Modulators
Tumor Cells, Cultured
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Summary: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. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00403-6