The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer
- Author
- FOLKES, Adrian J1 ; AHMADI, Khatereh1 ; FRIEDMAN, Lori S3 ; HAYES, Angela2 ; HANCOX, Timothy C1 ; KUGENDRADAS, Arumugam1 ; LENSUN, Letitia1 ; MOORE, Pauline1 ; OLIVERO, Alan G3 ; JODIE PANG3 ; PATEL, Sonal1 ; PERGL-WILSON, Giles H1 ; ALDERTON, Wendy K1 ; RAYNAUD, Florence I2 ; ROBSON, Anthony1 ; SAGHIR, Nahid1 ; SALPHATI, Laurent3 ; SOHAL, Sukhjit1 ; ULTSCH, Mark H3 ; VALENTI, Melanie2 ; WALLWEBER, Heidi J. A3 ; NAN CHI WAN1 ; WIESMANN, Christian3 ; ALIX, Sonia2 ; WORKMAN, Paul2 ; ZHYVOLOUP, Alexander1 ; ZVELEBIL, Marketa J4 ; SHUTTLEWORTH, Stephen J1 ; BAKER, Stewart J1 ; BOX, Gary2 ; CHUCKOWREE, Irina S1 ; CLARKE, Paul A2 ; DEPLEDGE, Paul1 ; ECCLES, Suzanne A2
[1] Piramed Pharma, 957 Buckingham Avenue, Slough, Berks SL1 4NL, United Kingdom
[2] Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddon Laboratories, Sutton, Surrey, SN2 5NG, United Kingdom
[3] Genentech, Inc., I DNA Way, South San Francisco, California 94080, United States
[4] Breakthrough Breast Cancer Research Centre, The Institute of Cancer Research, London, SW3 6JB, United Kingdom - Source
Journal of medicinal chemistry (Print). 2008, Vol 51, Num 18, pp 5522-5532, 11 p ; ref : 37 ref
- CODEN
- JMCMAR
- ISSN
- 0022-2623
- Scientific domain
- Pharmacology drugs
- Publisher
- American Chemical Society, Washington, DC
- Publication country
- United States
- Document type
- Article
- Language
- English
- Keyword (fr)
- 1-Phosphatidylinositol 3-kinase Animal Anticancéreux Biodisponibilité Cellule tumorale Chimiothérapie Cytotoxicité Dérivé de l'indazole Dérivé de la morpholine Dérivé de la pipérazine Glioblastome Homme In vitro In vivo Inhibiteur enzyme Lignée cellulaire Pharmacocinétique Relation structure activité Résistance hydrolyse Sulfonamide Synthèse chimique Sélectivité Transduction signal Voie orale GDC 0941 Lignée U87MG Thiéno[3,2-d]pyrimidine(2-indazol-4-yl-6-[(4-mésylpipérazino)méthyl]-4-morpholino) Thiénopyrimidine Cancer Enzyme Gliome malin Pathologie du système nerveux central Pathologie du système nerveux Traitement Transferases Tumeur maligne
- Keyword (en)
- 1-Phosphatidylinositol 3-kinase Animal Antineoplastic agent Bioavailability Tumor cell Chemotherapy Cytotoxicity Indazole derivatives Morpholine derivatives Piperazine derivatives Glioblastoma Human In vitro In vivo Enzyme inhibitor Cell line Pharmacokinetics Structure activity relation Hydrolysis resistance Sulfonamide Chemical synthesis Selectivity Signal transduction Oral administration Cancer Enzyme Malignant glioma Central nervous system disease Nervous system diseases Treatment Transferases Malignant tumor
- Keyword (es)
- 1-Phosphatidylinositol 3-kinase Animal Anticanceroso Biodisponibilidad Célula tumoral Quimioterapia Citotoxicidad Indazol derivado Piperazina derivado Glioblastoma Hombre In vitro In vivo Inhibidor enzima Línea celular Farmacocinética Relación estructura actividad Resistencia hidrólisis Sulfonamida Síntesis química Selectividad Transducción señal Vía oral Cáncer Enzima Glioma maligno Sistema nervosio central patología Sistema nervioso patología Tratamiento Transferases Tumor maligno
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02R Antineoplastic agents / 002B02R01 General aspects
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 20687106
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
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DOI
10.1021/jm800295d 
https://dx.doi.org/10.1021/jm800295d
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Europe PubMed Central access
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arXiv access
