Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3Kδ inhibitor

[Display omitted] Chemical optimization of the 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine (THPP) scaffold was conducted with a focus on cellular potency while maintaining high selectivity against PI3K isoforms. Compound 11f was identified as a potent, highly selective and orally available PI3Kδ inhib...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2019-03, Vol.27 (6), p.1056-1064
Hauptverfasser:	Hamajima, Toshihiro, Takahashi, Fumie, Kato, Koji, Sugano, Yukihito, Yamaki, Susumu, Suzuki, Daisuke, Moritomo, Ayako, Kubo, Satoshi, Nakamura, Koji, Yamagami, Kaoru, Yokoo, Koji, Fukahori, Hidehiko
Format:	Artikel
Sprache:	eng
Schlagworte:	5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidine Animals Cells, Cultured Class I Phosphatidylinositol 3-Kinases - antagonists & inhibitors Class I Phosphatidylinositol 3-Kinases - metabolism Female Humans Isoform selectivity Mice, Inbred BALB C Molecular Docking Simulation Phosphoinositide-3 Kinase Inhibitors - chemistry Phosphoinositide-3 Kinase Inhibitors - pharmacokinetics Phosphoinositide-3 Kinase Inhibitors - pharmacology PI3Kδ inhibitor Pyrrolidines - chemistry Pyrrolidines - pharmacokinetics Pyrrolidines - pharmacology
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