- Pyrazolopyrimidine compounds and preparation method thereof, and applications in preparation of anti-cancer drugs
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The invention provides a class of pyrazolopyrimidine compounds represented by a formula (I) or pharmaceutically acceptable salts thereof, and a preparation method thereof, and applications of the pyrazolopyrimidine compounds or the pharmaceutically accept
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Paragraph 0140-0147
(2020/04/17)
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- Regioselective Access to 3-Aryl-1-aminoisoquinolines via Nickel(I)-Catalyzed C-C and C-N Cascade Coupling Reactions from the Substituted 2-(Cyanomethyl)benzonitriles
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A novel and regioselective Ni(I) catalyzed C-C and C-N cascade coupling reactions has been developed. The cascade furnishes atom-economic access to 40 3-aryl-1-aminoisoquinolines. The regioselectivity of C(sp3)-cyano group over C(sp2
- Yang, Xicheng,Yu, Haihua,Xu, Yulong,Shao, Liming
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p. 9682 - 9695
(2018/09/06)
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- Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: A new class of inhibitors of lck kinase
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An imidazo[4,5-h]isoquinolin-7,9-dione (1) was identified as an adenosine 5′-triphosphate competitive inhibitor of lck by high throughput screening. Initial structure-activity relationship studies identified the dichlorophenyl ring and the imide NH as important pharmacophores. A binding model was constructed to understand how 1 binds to a related kinase, hck. These results suggested that removing the gem-dimethyl group and flattening the ring would enhance activity. This was realized by converting 1 to the imidazo[4,5-h]isoquinolin-9-one (20), resulting in an 18-fold improvement in potency against lck and a 50-fold increase in potency in a cellular assay.
- Snow, Roger J.,Cardozo, Mario G.,Morwick, Tina M.,Busacca, Carl A.,Dong, Yong,Eckner, Robert J.,Jacober, Stephen,Jakes, Scott,Kapadia, Suresh,Lukas, Susan,Panzenbeck, Maret,Peet, Gregory W.,Peterson, Jeffrey D.,Prokopowicz III, Anthony S.,Sellati, Rosemarie,Tolbert, Robert M.,Tschantz, Matt A.,Moss, Neil
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p. 3394 - 3405
(2007/10/03)
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