Design and Synthesis of 2-Heterocyclyl-3-arylthio-1H-indoles as Potent Tubulin Polymerization and Cell Growth Inhibitors with Improved Metabolic Stability

[Image: see text] New arylthioindoles (ATIs) were obtained by replacing the 2-alkoxycarbonyl group with a bioisosteric 5-membered heterocycle nucleus. The new ATIs 5, 8, and 10 inhibited tubulin polymerization, reduced cell growth of a panel of human transformed cell lines, and showed higher metabol...

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Main Authors: La Regina, Giuseppe, Bai, Ruoli, Rensen, Willeke, Coluccia, Antonio, Piscitelli, Francesco, Gatti, Valerio, Bolognesi, Alessio, Lavecchia, Antonio, Granata, Ilaria, Porta, Amalia, Maresca, Bruno, Soriani, Alessandra, Iannitto, Maria Luisa, Mariani, Marisa, Santoni, Angela, Brancale, Andrea, Ferlini, Cristiano, Dondio, Giulio, Varasi, Mario, Mercurio, Ciro, Hamel, Ernest, Lavia, Patrizia, Novellino, Ettore, Silvestri, Romano
Formato: Artigo
Idioma:Inglês
Publicado em: 2011
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3261769/
https://ncbi.nlm.nih.gov/pubmed/22044164
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm2012886
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