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.

Design, palladium-catalyzed synthesis, and biological investigation of 2-substituted 3-aroylquinolin-4(1H)-ones as inhibitors of the Hedgehog signaling pathway / Alfonsi, Romina; Botta, Bruno; Cacchi, Sandro; DI MARCOTULLIO, Lucia; Fabrizi, Giancarlo; Faedda, Roberta; Goggiamani, Antonella; Iazzetti, Antonia; Mori, Mattia. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - ELETTRONICO. - 60:(2017), pp. 1469-1477.

Design, palladium-catalyzed synthesis, and biological investigation of 2-substituted 3-aroylquinolin-4(1H)-ones as inhibitors of the Hedgehog signaling pathway.

ALFONSI, ROMINA;BOTTA, Bruno;CACCHI, Sandro;DI MARCOTULLIO, LUCIA;FABRIZI, Giancarlo;FAEDDA, ROBERTA;GOGGIAMANI, ANTONELLA
;
IAZZETTI, Antonia;
2017

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.
hedgehog pathway; hedgehog inhibitors; chemistry
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Design, palladium-catalyzed synthesis, and biological investigation of 2-substituted 3-aroylquinolin-4(1H)-ones as inhibitors of the Hedgehog signaling pathway / Alfonsi, Romina; Botta, Bruno; Cacchi, Sandro; DI MARCOTULLIO, Lucia; Fabrizi, Giancarlo; Faedda, Roberta; Goggiamani, Antonella; Iazzetti, Antonia; Mori, Mattia. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - ELETTRONICO. - 60:(2017), pp. 1469-1477.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/928720
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