Synthesis of pyrazoles and isoxazoles as potent α v β 3 receptor antagonists

TD Penning, A Khilevich, BB Chen, MA Russell…

文献索引：Penning, Thomas D.; Khilevich, Albert; Chen, Barbara B.; Russell, Mark A.; Boys, Mark L.; Wang, Yaping; Duffin, Tiffany; Engleman, V. Wayne; Finn, Mary Beth; Freeman, Sandra K.; Hanneke, Melanie L.; Keene, Jeffery L.; Klover, Jon A.; Nickols, G. Allen; Nickols, Maureen A.; Rader, Randall K.; Settle, Steven L.; Shannon, Kristen E.; Steininger, Christina N.; Westlin, Marisa M.; Westlin, William F. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 12 p. 3156 - 3161

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被引用次数: 44

摘要

We describe a series of pyrazole and isoxazole analogs as antagonists of the αvβ3 receptor. Compounds showed low to sub-nanomolar potency against αvβ3, as well as good selectivity against αIIbβ3. In HT29 cells, most analogs also demonstrated significant selectivity against αvβ6. Several compounds showed good pharmacokinetic properties in rats, in addition to anti-angiogenic activity in a mouse corneal micropocket model. Compounds were ...