期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 4, 页码 1469-1477出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b01135
关键词
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资金
- AIRC [IG14723]
- PRIN [2012C5YJSK002]
- Progetti di Ricerca di Universita Sapienza di Roma
- Pasteur Institute/Cenci Bolognetti Foundation
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.
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