369-26-6Relevant academic research and scientific papers
FUSED BICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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Paragraph 00196; 00229, (2019/03/05)
Fused bicyclic compounds and uses thereof in medicine. In particular, provided are fused bicyclic compounds used as ASK1 active regulator and and use of the compounds in the manufacture of a drug for treating a disease regulated by ASK1. Further provided are a pharmaceutical composition and a method of treating a disease regulated by ASK1 comprising administering the compounds or pharmaceutical composition thereof.
Substituent effects on the isomerization of hydrazone switches driven by the intramolecular hydrogen bond
Lu, Chaocao,Htan, Bu,Fu, Shitao,Ma, Chunmiao,Gan, Quan
, p. 4010 - 4016 (2019/07/03)
In this work, the substituent effects on hydrogen bonding in one kind of hydrazone-based switch are revealed. The E/Z isomerization ratios of these hydrazones and their intramolecular hydrogen bond strengths in the Z form were evaluated using NMR technique. Linear correlations between these parameters and Hammett empirical values for substituent effects are explored as well.
Oridonin derivatives as potential anticancer drug candidates triggering apoptosis through mitochondrial pathway in the liver cancer cells
Luo, Dongdong,Yi, Yujiao,Peng, Kai,Liu, Tangrong,Yang, Jiayu,Liu, Shan,Zhao, Wanzhou,Qu, Xianjun,Yu, Wengong,Gu, Yuchao,Wan, Shengbiao
, p. 365 - 379 (2019/06/17)
The biological function of the natural ent-kaurene diterpenoid isolated from genus Isodon, oridonin, has been intensively studied. However, its mechanism studies and clinical applications were hampered by its moderate biological activities. In order to en
Regioselective Synthesis of Angular Isocoumarinselenazoles: A Benzoselenazole-directed, Site-specific, Ruthenium-catalyzed C(sp2)-H Activation
Dhole, Sandip,Liao, Jen-Yu,Kumar, Sunil,Salunke, Deepak B.,Sun, Chung-Ming
, p. 942 - 950 (2018/01/22)
The synthesis of new, angular isocoumarinselenazoles is described, which involves the construction of 2-amino benzoselenazoles and their regioselective C2N-alkylation and alkyne insertion. An expeditious and metal-free synthesis of 2-aminobenzoselenazoles
COMPOUNDS AND COMPOSITIONS AS PDGFR KINASE INHIBITORS
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Page/Page column 68; 75, (2013/03/28)
The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase
Discovery of dabrafenib: A selective inhibitor of Raf Kinases with antitumor activity against B-Raf-driven tumors
Rheault, Tara R.,Stellwagen, John C.,Adjabeng, George M.,Hornberger, Keith R.,Petrov, Kimberly G.,Waterson, Alex G.,Dickerson, Scott H.,Mook, Robert A.,Laquerre, Sylvie G.,King, Alastair J.,Rossanese, Olivia W.,Arnone, Marc R.,Smitheman, Kimberly N.,Kane-Carson, Laurie S.,Han, Chao,Moorthy, Ganesh S.,Moss, Katherine G.,Uehling, David E.
supporting information, p. 358 - 362 (2013/05/09)
Hyperactive signaling of the MAP kinase pathway resulting from the constitutively active B-RafV600E mutated enzyme has been observed in a number of human tumors, including melanomas. Herein we report the discovery and biological evaluation of GSK2118436, a selective inhibitor of Raf kinases with potent in vitro activity in oncogenic B-Raf-driven melanoma and colorectal carcinoma cells and robust in vivo antitumor and pharmacodynamic activity in mouse models of B-RafV600E human melanoma. GSK2118436 was identified as a development candidate, and early clinical results have shown significant activity in patients with B-Raf mutant melanoma.
An efficient method for aryl nitro reduction and cleavage of azo compounds using iron powder/calcium chloride
Chandrappa,Vinaya,Ramakrishnappa,Rangappa
experimental part, p. 3019 - 3022 (2011/03/17)
A novel, efficient Fe/CaCl2 system is revealed for the reduction of nitroarenes and reductive cleavage of azo compounds by catalytic transfer hydrogenation (CTH). The selective reduction of nitro compounds in the presence of sensitive functional groups including halides, carbonyl, hydroxyl, aldehyde, methyl, methoxy, acetyl, nitrile, and ester substituents with an excellent yields is reported. The simple experimental procedure and easy purification make the protocol advantageous
BENZIMIDAZOLECARBOXAMIDES AS INHIBITORS OF FAK
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Page/Page column 62, (2010/11/17)
This invention relates to benzimadolecarboxamides of formula (I) which are inhibitors of focal adhesion kinase, and as such are useful for treating proliferative diseases
THIAZOLE AND OXAZOLE KINASE INHIBITORS
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Page/Page column 186, (2009/07/17)
The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
