Synthesis and SAR study of potent and selective PI3Kδ inhibitors

Bioorganic & Medicinal Chemistry Letters
2015.0

Abstract

2,3,4-Substituted quinolines such as (10a) were found to be potent inhibitors of PI3Kδ in both biochemical and cellular assays with good selectivity over three other class I PI3K isoforms. Some of those analogs showed favorable pharmacokinetic properties.

Knowledge Graph

Similar Paper

Synthesis and SAR study of potent and selective PI3Kδ inhibitors
Bioorganic & Medicinal Chemistry Letters 2015.0
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors
ACS Medicinal Chemistry Letters 2016.0
Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors
Bioorganic & Medicinal Chemistry 2018.0
Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3Kδ inhibitors
Bioorganic & Medicinal Chemistry 2019.0
Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors
Bioorganic & Medicinal Chemistry Letters 2017.0
Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation
MedChemComm 2019.0
Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors
Bioorganic & Medicinal Chemistry Letters 2019.0
Discovery of novel quinazolinone derivatives as high potent and selective PI3Kδ and PI3Kδ/γ inhibitors
European Journal of Medicinal Chemistry 2018.0
Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors
Bioorganic & Medicinal Chemistry Letters 2016.0
Discovery of a Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models
Journal of Medicinal Chemistry 2020.0