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Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy

Sonia Martı́nez, Sonsoles Rodríguez-Arístegui, Ana Isabel Hernández, Carmen Varela, Esther González Cantalapiedra, Rosa M. Álvarez, Antonio R. Hergueta, James R. Bischoff, María I. Albarrán, Antonio Cebriá,

Bioorganic & Medicinal Chemistry Letters · 2017 · 10 citations · 20 references

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Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

Yung-Chi Cheng, William H. Prusoff · Biochemical Pharmacology · 1973 · 12.9K citations

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Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent <i>in vivo</i> antitumor activity

Sauveur-Michel Maira, Frédéric Stauffer, Josef Brueggen et al. · Molecular Cancer Therapeutics · 2008 · 1.1K citations · Full text

, , +13

The Identification of 2-(1<i>H</i>-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-<i>d</i>]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer

Adrian Folkes, Khatereh Ahmadi, W. Alderton et al. · Journal of Medicinal Chemistry · 2008 · 746 citations · Full text

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Mutations in a signalling pathway

D. Williams Parsons, Tian‐Li Wang, Yardena Samuels et al. · Nature · 2005 · 634 citations · Full text

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The Structure of a Human p110α/p85α Complex Elucidates the Effects of Oncogenic PI3Kα Mutations

Chuan‐Hsiang Huang, Diana Mandelker, Oleg Schmidt‐Kittler et al. · Science · 2007 · 561 citations

, , +15