854632-98-7Relevant articles and documents
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides
Laufer, Radoslaw,Ng, Grace,Liu, Yong,Patel, Narendra Kumar B.,Edwards, Louise G.,Lang, Yunhui,Li, Sze-Wan,Feher, Miklos,Awrey, Don E.,Leung, Genie,Beletskaya, Irina,Plotnikova, Olga,Mason, Jacqueline M.,Hodgson, Richard,Wei, Xin,Mao, Guodong,Luo, Xunyi,Huang, Ping,Green, Erin,Kiarash, Reza,Lin, Dan Chi-Chia,Harris-Brandts, Marees,Ban, Fuqiang,Nadeem, Vincent,Mak, Tak W.,Pan, Guohua J.,Qiu, Wei,Chirgadze, Nickolay Y.,Pauls, Henry W.
, p. 4968 - 4997 (2014/10/16)
TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50 = 3.6 nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described.
Novel organophosphorus derivatives of indazoles and use thereof as medicinal products
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Page/Page column 10; 11, (2008/06/13)
The present invention relates in particular to novel chemical compounds, particularly to novel organophosphorus derivatives of indazoles, to the compositions containing them, and to the use thereof as medicinal products for treating cancers.
