1232935-44-2Relevant articles and documents
Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists
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
scheme or table, p. 3618 - 3622 (2010/09/04)
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 representative compound from this class demonstrated significant tumor volume reduction in a mouse medulloblastoma model.
