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, Joseph F. III published an article in Journal of Medicinal Chemistry. The title of the article was 《1-Amino-4-benzylphthalazines as Orally Bioavailable Smoothened Antagonists with Antitumor Activity》.Application of 1057682-05-9 The author mentioned the following in the article:
Abnormal activation of the Hedgehog (Hh) signaling pathway has been linked to several types of human cancers, and the development of small-mol. 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, e.g. I, that act via antagonism of the Smoothened receptor. A variety of analogs 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. After reading the article, we found that the author used (R)-6-(3-Methylpiperazin-1-yl)nicotinonitrile(cas: 1057682-05-9Application of 1057682-05-9)
(R)-6-(3-Methylpiperazin-1-yl)nicotinonitrile(cas: 1057682-05-9) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Application of 1057682-05-9
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics