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 originale | English |
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pagine (da-a) | 1469-1477 |
Numero di pagine | 9 |
Rivista | Journal of Medicinal Chemistry |
Volume | 60 |
DOI | |
Stato di pubblicazione | Pubblicato - 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