209971-43-7Relevant articles and documents
AROMATIC RING COMPOUND
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Paragraph 0297, (2015/03/28)
The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K
Pecchi, Sabina,Ni, Zhi-Jie,Han, Wooseok,Smith, Aaron,Lan, Jiong,Burger, Matthew,Merritt, Hanne,Wiesmann, Marion,Chan, John,Kaufman, Susan,Knapp, Mark S.,Janssen, Johanna,Huh, Kay,Voliva, Charles F.
supporting information, p. 4652 - 4656 (2013/08/23)
PI3 kinases are a family of lipid kinases mediating numerous cell processes such as proliferation, migration and differentiation. The PI3 Kinase pathway is often de-regulated in cancer through PI3Kα overexpression, gene amplification, mutations and PTEN p
Fragment based discovery of a novel and selective PI3 kinase inhibitor
Hughes, Samantha J.,Millan, David S.,Kilty, Iain C.,Lewthwaite, Russell A.,Mathias, John P.,Reilly, Mark A.O.,Pannifer, Andrew,Phelan, Anne,Stühmeier, Frank,Baldock, Darren A.,Brown, David G.
scheme or table, p. 6586 - 6590 (2011/12/04)
We report the use of fragment screening and fragment based drug design to develop a PI3c kinase fragment hit into a lead. Initial fragment hits were discovered by high concentration biochemical screening, followed by a round of virtual screening to identify additional ligand efficient fragments. These were developed into potent and ligand efficient lead compounds using structure guided fragment growing and merging strategies. This led to a potent, selective, and cell permeable PI3c kinase inhibitor with good metabolic stability that was useful as a preclinical tool compound.