Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists

…, MG Johnson, JA Kaizerman, G Lee, DL McMinn…

文献索引：Lucas, Brian S.; Aaron, Wade; An, Songzhu; Austin, Richard J.; Brown, Matthew; Chan, Hon; Chong, Angela; Hungate, Randall; Huang, Tom; Jiang, Ben; Johnson, Michael G.; Kaizerman, Jacob A.; Lee, Gary; McMinn, Dustin L.; Orf, Jessica; Powers, Jay P.; Rong, Minqing; Toteva, Maria M.; Uyeda, Craig; Wickramasinghe, Dineli; Xu, Guifen; Ye, Qiuping; Zhong, Wendy Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 12 p. 3618 - 3622

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被引用次数: 15

摘要

The Hedgehog (Hh) signaling pathway regulates cell proliferation and differentiation in developing tissues, and abnormal activation of the Hh pathway has been linked to several tumor subsets. As a transducer of Hh signaling, the GPCR-like protein Smoothened (Smo) is a promising target for disruption of unregulated Hh signaling. A series of 1-amino-4- arylphthalazines was developed as potent and orally bioavailable inhibitors of Smo. A ...