917474-59-0Relevant articles and documents
1-(5-Carboxyindazol-1-yl)propan-2-ones as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase: bioisosteric replacement of the carboxylic acid moiety
Althaus, Jan,Hake, Theresa,Hanekamp, Walburga,Lehr, Matthias
, p. 131 - 140 (2016)
Indazole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position 1 were previously reported to be potent dual inhibitors of cytosolic phospholipase A2α (cPLA2α) and fatty acid amide hydrolase (FAAH). In continuation of our structure-activity studies on cPLA2α and FAAH inhibitors, a number of derivatives of these substances characterized by bioisosteric replacement of the carboxylic acid functionality by inverse amides, sulfonylamides, carbamates and ureas were prepared. The biological evaluation of the obtained compounds showed that the carboxylic acid functionality of the lead compounds is of special importance for a pronounced inhibition of cPLA2α and FAAH.
The discovery of orally bioavailable tyrosine threonine kinase (TTK) inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as anticancer agents
Liu, Yong,Lang, Yunhui,Patel, Narendra Kumar,Ng, Grace,Laufer, Radoslaw,Li, Sze-Wan,Edwards, Louise,Forrest, Bryan,Sampson, Peter B.,Feher, Miklos,Ban, Fuqiang,Awrey, Donald E.,Beletskaya, Irina,Mao, Guodong,Hodgson, Richard,Plotnikova, Olga,Qiu, Wei,Chirgadze, Nickolay Y.,Mason, Jacqueline M.,Wei, Xin,Lin, Dan Chi-Chia,Che, Yi,Kiarash, Reza,Madeira, Brian,Fletcher, Graham C.,Mak, Tak W.,Bray, Mark R.,Pauls, Henry W.
supporting information, p. 3366 - 3392 (2015/05/05)
The acetamido and carboxamido substituted 3-(1H-indazol-3-yl)benzenesulfonamides are potent TTK inhibitors. However, they display modest ability to attenuate cancer cell growth; their physicochemical properties, and attendant pharmacokinetic parameters, a
INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 115, (2013/04/25)
The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as T