1534350-44-1Relevant academic research and scientific papers
Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core
Němec, Václav,Maier, Luká?,Berger, Benedict-Tilman,Chaikuad, Apirat,Drápela, Stanislav,Sou?ek, Karel,Knapp, Stefan,Paruch, Kamil
, (2021)
The furo [3,2-b]pyridine motif represents a relatively underexplored central pharmacophore in the area of kinase inhibitors. Herein, we report flexible synthesis of 3,5-disubstituted furo [3,2-b]pyridines that relies on chemoselective couplings of newly prepared 5-chloro-3-iodofuro [3,2-b]pyridine. This methodology allowed efficient second-generation synthesis of the state-of-the-art chemical biology probe for CLK1/2/4 MU1210, and identification of the highly selective inhibitors of HIPKs MU135 and MU1787 which are presented and characterized in this study, including the X-ray crystal structure of MU135 in HIPK2. chemical biology probe
Design, synthesis and biological evaluation of 1H-indazole derivatives as novel ASK1 inhibitors
Hou, Shaohua,Yang, Xiping,Yang, Yuejing,Tong, Yu,Chen, Quanwei,Wan, Boheng,Wei, Ran,Lu, Tao,Chen, Yadong,Hu, Qinghua
, (2021/05/10)
Apoptosis signal-regulating kinase 1 (ASK1, MAP3K5), a member of the mitogen-activated protein kinase (MAPK) signaling pathway, is involved in cell survival, differentiation, stress response, and apoptosis. ASK1 kinase inhibition has emerged as a promisin
A modular synthesis of functionalised phenols enabled by controlled boron speciation
Molloy, John J.,Law, Robert P.,Fyfe, James W. B.,Seath, Ciaran P.,Hirst, David J.,Watson, Allan J. B.
supporting information, p. 3093 - 3102 (2015/04/27)
A modular synthesis of functionalised biaryl phenols from two boronic acid derivatives has been developed via one-pot Suzuki-Miyaura cross-coupling, chemoselective control of boron solution speciation to generate a reactive boronic ester in situ, and oxidation. The utility of this method has been further demonstrated by application in the synthesis of drug molecules and components of organic electronics, as well as within iterative cross-coupling.
PYRIMIDINE PYRAZOLYL DERIVATIVES
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Page/Page column 111; 112, (2014/02/15)
The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases (I).
