209971-46-0Relevant academic research and scientific papers
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.
, p. 6586 - 6590 (2011)
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.
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.
, 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
Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors
Terao, Yoshito,Suzuki, Hideo,Yoshikawa, Masato,Yashiro, Hiroaki,Takekawa, Shiro,Fujitani, Yasushi,Okada, Kengo,Inoue, Yoshihisa,Yamamoto, Yoshio,Nakagawa, Hideyuki,Yao, Shuhei,Kawamoto, Tomohiro,Uchikawa, Osamu
, p. 7326 - 7329 (2013/02/21)
Imidazo[1,2-a]pyridine derivatives were designed, synthesized, and evaluated as inhibitors of the apoptosis signal-regulating kinase 1 (ASK1). These were based on a benzothiazole derivative that was discovered from high-throughput screening of our compound library. As a result, we identified potent, selective, and orally bioavailable ASK1 inhibitors for wide range of therapeutic targets.
Chemoselective arylsulfenylation of 2-aminoimidazo[1,2-α]pyridines by phenyliodine(III) bis(trifiuoroacetate) (PIFA)
Hamdouchi, Chafiq,Sanchez, Concha,Ezquerra, Jesus
, p. 867 - 872 (2007/10/03)
A series of 2-(trifluoroacetamido)imidazo[1,2-a]pyridines was prepared and treated with phenyliodine(III) bis(trifluoroacetate) (PIFA) in the presence of a variety of thiols leading chemoselectively to the corresponding 3-sulfides. Exposure of these adducts to silica gel in MeOH/CH2Cl2 provides a convenient method for the cleavage of the trifluoroacetamide group.
