371244-06-3Relevant academic research and scientific papers
Atropisomerism and Conformational Equilibria: Impact on PI3Kδ Inhibition of 2-((6-Amino-9H-purin-9-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one (IC87114) and Its Conformationally Restricted Analogs
Lodola, Alessio,Bertolini, Serena,Biagetti, Matteo,Capacchi, Silvia,Facchinetti, Fabrizio,Gallo, Paola Maria,Pappani, Alice,Mor, Marco,Pala, Daniele,Rivara, Silvia,Visentini, Filippo,Corsi, Mauro,Capelli, Anna Maria
, p. 4304 - 4315 (2017)
IC87114 [compound 1, (2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one)] is a potent PI3K inhibitor selective for the δ isoform. As predicted by molecular modeling calculations, rotation around the bond connecting the quinazolin-
INHIBITORS OF PI3K-DELTA AND METHODS OF THEIR USE AND MANUFACTURE
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, (2012/04/04)
The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds
METHODS AND COMPOSITIONS FOR TREATMENT OF OPHTHALMIC CONDITIONS
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, (2011/11/12)
The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating signal transduction by certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PB kinase in a
A novel highly stereoselective synthesis of 2,3-disubstituted 3H-quinazoline-4-one derivatives
Zhichkin, Paul,Kesicki, Edward,Treiberg, Jennifer,Bourdon, Lisa,Ronsheim, Matthew,Ooi, Hua Chee,White, Stephen,Judkins, Angela,Fairfax, David
, p. 1415 - 1418 (2007/10/03)
Figure presented An efficient three-step synthesis of chiral 3H-quinazoline-4-one derivatives from commercial materials is disclosed. The Mumm reaction of imidoyl chloride with α-amino acids followed by reductive cyclization affords enantiomerically pure (ee >93%) quinazoline-4-ones in good overall yield. A comparison with existing approaches indicates that this method is superior for hindered substrates.
Inhibitors of human phosphatidylinositol 3-kinase delta
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Page column 65-66, (2008/06/13)
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.
