Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer

[Image: see text] Phosphoinositide-3-kinases (PI3Ks) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein we describe the structure guided optimization of a series of 2-morpholino, 4-substituted, 6-heterocyclic pyrimidines where...

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Hauptverfasser: Burger, Matthew T., Pecchi, Sabina, Wagman, Allan, Ni, Zhi-Jie, Knapp, Mark, Hendrickson, Thomas, Atallah, Gordana, Pfister, Keith, Zhang, Yanchen, Bartulis, Sarah, Frazier, Kelly, Ng, Simon, Smith, Aaron, Verhagen, Joelle, Haznedar, Joshua, Huh, Kay, Iwanowicz, Ed, Xin, Xiaohua, Menezes, Daniel, Merritt, Hanne, Lee, Isabelle, Wiesmann, Marion, Kaufman, Susan, Crawford, Kenneth, Chin, Michael, Bussiere, Dirksen, Shoemaker, Kevin, Zaror, Isabel, Maira, Sauveur-Michel, Voliva, Charles F.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2011
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4017971/
https://ncbi.nlm.nih.gov/pubmed/24900266
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml200156t
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