13177-71-4Relevant articles and documents
1-Amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity
Miller-Moslin, Karen,Peukert, Stefan,Jain, Rishi K.,McEwan, Michael A.,Karki, Rajesh,Llamas, Luis,Yusuff, Naeem,He, Feng,Li, Yanhong,Sun, Yingchuan,Dai, Miao,Perez, Lawrence,Michael, Walter,Sheng, Tao,Lei, Huangshu,Zhang, Rui,Williams, Juliet,Bourret, Aaron,Ramamurthy, Arun,Yuan, Jing,Guo, Ribo,Matsumoto, Melissa,Vattay, Anthony,Maniara, Wieslawa,Amaral, Adam,Dorsch, Marion,Kelleher III, Joseph F.
experimental part, p. 3954 - 3968 (2010/01/16)
Abnormal activation of the Hedgehog (Hh) signaling pathway has been linked to several types of human cancers, and the development of small-molecule inhibitors of this pathway represents a promising route toward novel anticancer therapeutics. A cell-based screen performed in our laboratories identified a new class of Hh pathway inhibitors, 1-amino-4-benzylphthalazines, that act via antagonism of the Smoothened receptor. A variety of analogues were synthesized and their structure-activity relationships determined. This optimization resulted in the discovery of high affinity Smoothened antagonists, one of which was further profiled in vivo. This compound displayed a good pharmacokinetic profile and also afforded tumor regression in a genetic mouse model of medulloblastoma.
ORGANIC COMPOUNDS AND THEIR USES
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Page/Page column 116, (2008/12/07)
The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula (I).
Substituted pyridines and pyridazines with angiogenesis inhibiting activity
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Page column 52, (2010/02/05)
Substituted pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R1and R2may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents. Pharmaceutical compositions containing these materials, and methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using these materials are also disclosed.