New synthetic approach to paullones and characterization of their SIRT1 inhibitory activity (Articolo in rivista)

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Label
  • New synthetic approach to paullones and characterization of their SIRT1 inhibitory activity (Articolo in rivista) (literal)
Anno
  • 2012-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1039/c2ob06695e (literal)
Alternative label
  • Soto, Sara; Vaz, Esther; Dell'Aversana, Carmela; Alvarez, Rosana; Altucci, Lucia; de Lera, Angel R. (2012)
    New synthetic approach to paullones and characterization of their SIRT1 inhibitory activity
    in Organic & biomolecular chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Soto, Sara; Vaz, Esther; Dell'Aversana, Carmela; Alvarez, Rosana; Altucci, Lucia; de Lera, Angel R. (literal)
Pagina inizio
  • 2101 (literal)
Pagina fine
  • 2112 (literal)
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  • 10 (literal)
Rivista
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  • PMID: 22286328 (literal)
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  • 12 (literal)
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  • 10 (literal)
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  • E pub (literal)
Note
  • ISI Web of Science (WOS) (literal)
  • ISI Web of Science (WoS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • University of Vigo; Seconda Universita degli Studi di Napoli; CNR IGB (literal)
Titolo
  • New synthetic approach to paullones and characterization of their SIRT1 inhibitory activity (literal)
Abstract
  • A series of 7,12-dihydroindolo[3,2-d][1] benzazepine-6(5H)-ones (paullones) substituted at C9/C10 (Br) and C2 (Me, CF3, CO2Me) have been synthesized by a one-pot Suzuki-Miyaura cross-coupling of an o-aminoarylboronic acid and methyl 2-iodoindoleacetate followed by intramolecular amide formation. Other approaches to the paullone scaffold based on Pd-catalyzed C-H activation were unsuccessful. In vitro enzymatic assay with recombinant human SIRT-1 indicated a strong inhibitory profile for the series, in particular the analogue with a methoxycarbonyl group at C2 and a bromine at C9. These compounds are, in general, inducers of granulocyte differentiation of the U937 acute leukemia cell line and cause a marked increase in pre-G1 of the cell cycle. (literal)
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