68700-92-5Relevant articles and documents
QUINOLINE DERIVATIVES AS SMO INHIBITORS
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Paragraph 0665; 0666, (2017/02/28)
Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
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.
Substituted 11-oxo-11H-pyrido[2,1-b]quinazolines and method of inhibiting allergic reactions with them
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, (2008/06/13)
Pyrido[2,1-b]quinazolines of the formulas STR1 wherein R1, R1 ', R2, R2 ', R3, R3 ', R4 and R10 are as hereinafter set forth, and processes for the preparation thereof