Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase γ (PI3Kγ)

Phosphoinositide-3-kinase γ (PI3Kγ) is highly expressed in immune cells and promotes the production and migration of inflammatory mediators. The inhibition of PI3Kγ has been shown to repolarize the tumor immune microenvironment to a more inflammatory phenotype, thereby controlling immune suppression...

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Veröffentlicht in:	Journal of medicinal chemistry 2022-01, Vol.65 (2), p.1418-1444
Hauptverfasser:	Mata, Guillaume, Miles, Dillon H, Drew, Samuel L, Fournier, Jeremy, Lawson, Kenneth V, Mailyan, Artur K, Sharif, Ehesan U, Yan, Xuelei, Beatty, Joel W, Banuelos, Jesus, Chen, Jie, Ginn, Elaine, Chen, Ada, Gerrick, Kimberline Y, Pham, Amber T, Wong, Kent, Soni, Divyank, Dhanota, Puja, Shaqfeh, Stefan G, Meleza, Cesar, Narasappa, Nell, Singh, Hema, Zhao, Xiaoning, Jin, Lixia, Schindler, Ulrike, Walters, Matthew J, Young, Stephen W, Walker, Nigel P, Leleti, Manmohan Reddy, Powers, Jay P, Jeffrey, Jenna L
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemistry Animals Class Ib Phosphatidylinositol 3-Kinase - chemistry Drug Design Drug Discovery Humans Male Molecular Docking Simulation Phosphoinositide-3 Kinase Inhibitors - pharmacology Pyrimidines - chemistry Rats Rats, Sprague-Dawley Structure-Activity Relationship
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