29528-25-4Relevant articles and documents
Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946)
Scott, William J.,Hentemann, Martin F.,Rowley, R. Bruce,Bull, Cathy O.,Jenkins, Susan,Bullion, Ann M.,Johnson, Jeffrey,Redman, Anikó,Robbins, Arthur H.,Esler, William,Fracasso, R. Paul,Garrison, Timothy,Hamilton, Mark,Michels, Martin,Wood, Jill E.,Wilkie, Dean P.,Xiao, Hong,Levy, Joan,Stasik, Enrico,Liu, Ningshu,Schaefer, Martina,Brands, Michael,Lefranc, Julien
, p. 1517 - 1530 (2016/08/27)
The phosphoinositide 3-kinase (PI3K) pathway is aberrantly activated in many disease states, including tumor cells, either by growth factor receptor tyrosine kinases or by the genetic mutation and amplification of key pathway components. A variety of PI3K isoforms play differential roles in cancers. As such, the development of PI3K inhibitors from novel compound classes should lead to differential pharmacological and pharmacokinetic profiles and allow exploration in various indications, combinations, and dosing regimens. A screening effort aimed at the identification of PI3Kγ inhibitors for the treatment of inflammatory diseases led to the discovery of the novel 2,3-dihydroimidazo[1,2-c]quinazoline class of PI3K inhibitors. A subsequent lead optimization program targeting cancer therapy focused on inhibition of PI3Kα and PI3Kβ. Herein, initial structure–activity relationship findings for this class and the optimization that led to the identification of copanlisib (BAY 80-6946) as a clinical candidate for the treatment of solid and hematological tumors are described.
Clay-supported 2-phenyl-1H-imidazole derivatives for heterogeneous catalysis of Henry reaction
Holesova, Sylva,Paaik, Patrik,Ludwig, Miroslav
body text, p. 907 - 914 (2011/10/04)
Figure represented. Six derivatives (1-6) of 2-phenyl-1H-imidazole were tested as catalysts of Henry reaction. Three new (4-6) 2-phenyl-1H-imidazole derivatives, differently substituted (thio)ureas, were synthesized and determined by 1H NMR and
Heterocyclic Compounds with a Bridgehead Nitrogen Atom. Synthesis in the Imidazoquinazoline Series
Gueiffier, A.,Viols, H.,Chapat, J. P.,Chavignon, O.,Teulade, J. C.,Dauphin, G.
, p. 421 - 425 (2007/10/02)
The structures of imidazoquinazolines were reexaminated and established by spectroscopic studies with the aid of high-field 1H and 13C nmr and mass spectra.In acidic media, 3 reacts to give the products of electrophilic substitution reaction and ring opening compound 5, leading to the imidazobenzotriazine ring.
