Design, Palladium-Catalyzed Synthesis, and Biological Investigation of 2-Substituted 3-Aroylquinolin-4(1H)-ones as Inhibitors of the Hedgehog Signaling Pathway

Romina Alfonsi, Bruno Botta, Sandro Cacchi, Lucia Di Marcotullio, Giancarlo Fabrizi, Roberta Faedda, Antonella Goggiamani*, Antonia Iazzetti, Mattia Mori

*Autore corrispondente per questo lavoro

Risultato della ricerca: Contributo in rivistaArticolo in rivista

Abstract

2-Substituted 3-aroylquinolin-4(1H)-ones, prepared through a palladium-catalyzed carbonylative cyclization of N-(2-iodoaryl)enaminones, proved to inhibit efficiently the Hedgehog pathway through direct antagonism of the wild-type and drug-resistant form of the Smoothened receptor. Notably, these compounds repressed the Hh-dependent growth events and the proliferation of tumor cells with aberrant activation of the Hh pathway, which plays a crucial role in development and tumorigenesis.
Lingua originaleEnglish
pagine (da-a)1469-1477
Numero di pagine9
RivistaJournal of Medicinal Chemistry
Volume60
DOI
Stato di pubblicazionePubblicato - 2017

Keywords

  • Animals
  • Antineoplastic Agents
  • Catalysis
  • Cell Line
  • Cell Line, Tumor
  • Cell Proliferation
  • Drug Design
  • Hedgehog Proteins
  • Humans
  • Mice
  • Models, Molecular
  • Neoplasms
  • Palladium
  • Quinolones
  • Signal Transduction

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