387358-27-2Relevant articles and documents
Fluorinated adenosine A2A receptor antagonists inspired by preladenant as potential cancer immunotherapeutics
Yuan, Gengyang,Jankins, Tanner C.,Patrick, Christopher G.,Philbrook, Phaethon,Sears, Olivia,Hatfield, Stephen,Sitkovsky, Michail,Vasdev, Neil,Liang, Steven H.,Ondrechen, Mary Jo,Pollastri, Michael P.,Jones, Graham B.
, (2018/10/20)
Antagonism of the adenosine A2A receptor on T cells blocks the hypoxia-adenosinergic pathway to promote tumor rejection. Using an in vivo immunoassay based on the Concanavalin A mouse model, a series of A2A antagonists were studied and identified preladenant as a potent lead compound for development.Molecular modeling was employed to assist drug design and subsequent synthesis of analogs and those of tozadenant, including fluorinated polyethylene glycol PEGylated derivatives. The efficacy of the analogs was evaluated using two in vitro functional bioassays, and compound 29, a fluorinated triethylene glycol derivative of preladenant, was confirmed as a potential immunotherapeutic agent.
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists
Silverman, Lisa S.,Caldwell, John P.,Greenlee, William J.,Kiselgof, Eugenia,Matasi, Julius J.,Tulshian, Deen B.,Arik, Leyla,Foster, Carolyn,Bertorelli, Rosalia,Monopoli, Angela,Ongini, Ennio
, p. 1659 - 1662 (2007/10/03)
A novel series of 3-substituted-8-aryl-[1,2,4]-triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine A2A receptor antagonists with improved selectivity over the A1 receptor, physiochemical properties, and pharmacokinetic profiles as compared to those of Sch 58261. As a result of structural modifications, numerous analogs with excellent in vitro binding affinities and selectivities were identified. Moreover, compound 27 displayed both superior in vitro and highly promising in vivo profiles.
