Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kδ inhibitors.

[1]  J. Chandrasekhar,et al.  2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors. , 2016, Journal of medicinal chemistry.

[2]  Igor M. Prokopczyk,et al.  Hydrogen Bond Basicity Prediction for Medicinal Chemistry Design. , 2016, Journal of medicinal chemistry.

[3]  J. McCarter,et al.  Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors. , 2016, Journal of medicinal chemistry.

[4]  S. Green,et al.  Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. , 2015, Bioorganic & medicinal chemistry letters.

[5]  P. Jones,et al.  Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease. , 2015, Journal of medicinal chemistry.

[6]  Paul Workman,et al.  Drugging PI3K in cancer: refining targets and therapeutic strategies , 2015, Current opinion in pharmacology.

[7]  S. Green,et al.  Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold. , 2015, Bioorganic & medicinal chemistry letters.

[8]  J. R. Somoza,et al.  The characterization of idelalisib binding to PI3Kδ 1 Structural, biochemical and biophysical characterization of idelalisib binding to phosphoinositide 3-kinase delta* , 2015 .

[9]  Xiaolin Hao,et al.  Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. , 2015, Journal of medicinal chemistry.

[10]  Sungwoo Hong,et al.  Selective and potent small-molecule inhibitors of PI3Ks. , 2014, Future medicinal chemistry.

[11]  Bonnie Tillotson,et al.  PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. , 2013, Chemistry & biology.

[12]  Doriano Fabbro,et al.  Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. , 2013, Bioorganic & medicinal chemistry letters.

[13]  Steve Price,et al.  Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf. , 2013, Bioorganic & medicinal chemistry letters.

[14]  Anaïs F. M. Noisier,et al.  Discovery and application of iminotriphenylphosphorane as a formal aromatic primary amine protecting group , 2012 .

[15]  P. Savy,et al.  Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition. , 2012, Journal of medicinal chemistry.

[16]  Janet L. Smith,et al.  Targeting phosphoinositide 3-kinase δ for allergic asthma. , 2012, Biochemical Society transactions.

[17]  David W. Johnson,et al.  CAL-101 (GS-1101), a Specific Inhibitor of Phosphatidylinositol-3-Kinase-Delta (PI3Kδ), Disrupts Signals From the Microenvironment, Induces Apoptosis, and Enhances the Antitumor Activity of Everolimus (RAD001), An Inhibitor of Mammalian Target of Rapamycin (mTOR), in Mantle Cell Lymphoma (MCL), , 2011 .

[18]  Yi Liu,et al.  The p110δ crystal structure uncovers mechanisms for selectivity and potency of novel PI3K inhibitors , 2009, Nature chemical biology.

[19]  Jennifer D. Venable,et al.  Small molecule inhibitors of phosphoinositide 3-kinase (PI3K) delta and gamma. , 2009, Current topics in medicinal chemistry.

[20]  Emilio Hirsch,et al.  Blockade of PI3Kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis , 2005, Nature Medicine.

[21]  Roger L. Williams,et al.  Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine. , 2000, Molecular cell.