1374969-99-9Relevant academic research and scientific papers
Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity
Taniguchi, Toru,Inagaki, Hiroaki,Baba, Daichi,Yasumatsu, Isao,Toyota, Akiko,Kaneta, Yasuyuki,Kiga, Masaki,Iimura, Shin,Odagiri, Takashi,Shibata, Yoshihiro,Ueda, Kiyono,Seo, Maki,Shimizu, Hiroki,Imaoka, Tomoki,Nakayama, Kiyoshi
, p. 737 - 742 (2019)
To obtain a new anticancer drug, we focused on FER tyrosine kinase. Starting with high-throughput screening with our in-house chemical library, compound 1, which has a pyridine moiety, was found. Referring to their X-ray crystal structure with FES proto-oncogene tyrosine kinase, as a surrogate of FER followed by chemical modification including scaffold hopping of the pyridine template, we discovered pyrido-pyridazinone derivatives with potent FER kinase inhibitory activity. Here, we disclose the structure-activity relationship on the scaffold and representative compound 21 (DS21360717), which showed in vivo antitumor efficacy in a subcutaneous tumor model.
BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS
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Page/Page column 147, (2012/05/20)
The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
