2-Arylidenedihydroindole-3-ones: design, synthesis, and biological activity on bladder carcinoma cell lines |
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Authors: | Gerby Bastien Boumendjel Ahcène Blanc Madeleine Bringuier Pierre Paul Champelovier Pierre Fortuné Antoine Ronot Xavier Boutonnat Jean |
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Institution: | Laboratoire de Dynamique Cellulaire, EPHE, UMR-CNRS 5525, IFRT 130, Université Joseph Fourier, Pavillon Taillefer, 38706 La Tronche Cedex, France. |
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Abstract: | 2-Arylidenedihydroindole-3-ones were assayed for their antiproliferative and apoptotic abilities as potential drug candidates to treat bladder tumor. These compounds were tested on cell lines obtained from bladder tumors of various stages superficial (pTa and pT1) vs. invasive (pT2)]. The most active compound (3c) inhibited the proliferation, induced apoptosis, and decreased the expression of p-Stat5 and p-Pyk2 in DAG-1 and RT112 lines in which the FGFR3 is either mutated or overexpressed. Knowing that FGFR3 is involved in cell proliferation, differentiation, and migration through cell signaling pathways including p-Stat5 way via p-Pyk2, let us assume that compound 3c may probably act through FGFR3 pathway. |
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