65971-74-6Relevant articles and documents
Saccharomonosporine A inspiration; synthesis of potent analogues as potential PIM kinase inhibitors
Abdel-Rahman, Hamdy M.,Abdelmohsen, Usama Ramadan,Aboulmagd, Asmaa M.,Hassan, Hossam M.,Sayed, Ahmed M.
, p. 6752 - 6762 (2020/03/03)
Saccharomonosporine A was recently reported as a natural anti-cancer agent working through inhibition of a Proviral integration site for Moloney murine leukemia virus-1 (PIM-1) kinase. Structural bioisosteres of this natural product were synthesized and t
Indolone compound as well as preparation method and application thereof
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Paragraph 0012; 0018, (2019/04/17)
The invention relates to an indolone compound, which is 1-(4-chlorobenzyl)-3-(hydroxyimino)-4-(4-(trifluoromethyl)phenyl)-dihydroindol-2-one. The indolone compound can be used for effectively inhibiting the activity of an hTERT gene promoter; shown by a s
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4
Cheung, Mui,Bao, Weike,Behm, David J.,Brooks, Carl A.,Bury, Michael J.,Dowdell, Sarah E.,Eidam, Hilary S.,Fox, Ryan M.,Goodman, Krista B.,Holt, Dennis A.,Lee, Dennis,Roethke, Theresa J.,Willette, Robert N.,Xu, Xiaoping,Ye, Guosen,Thorneloe, Kevin S.
supporting information, p. 549 - 554 (2017/05/19)
Transient Receptor Potential Vanilloid 4 (TRPV4) is a member of the Transient Receptor Potential (TRP) superfamily of cation channels. TRPV4 is expressed in the vascular endothelium in the lung and regulates the integrity of the alveolar septal barrier. Increased pulmonary vascular pressure evokes TRPV4-dependent pulmonary edema, and therefore, inhibition of TRPV4 represents a novel approach for the treatment of pulmonary edema associated with conditions such as congestive heart failure. Herein we report the discovery of an orally active, potent, and selective TRPV4 blocker, 3-(1,4′-bipiperidin-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide (GSK2193874, 28) after addressing an unexpected off-target cardiovascular liability observed from in vivo studies. GSK2193874 is a selective tool for elucidating TRPV4 biology both in vitro and in vivo.