1-Amino-4-benzylphthalazines as Orally Bioavailable Smoothened Antagonists with Antitumor Activity
- Author
- MILLER-MOSLIN, Karen1 ; PEUKERT, Stefan1 ; MIAO DAI1 ; PEREZ, Lawrence1 ; MICHAEL, Walter1 ; TAO SHENG1 ; HUANGSHU LEI1 ; RUI ZHANG1 ; WILLIAMS, Juliet3 ; BOURRET, Aaron2 ; RAMAMURTHY, Arun2 ; JING YUAN3 ; JAIN, Rishi K1 ; RIBO GUO3 ; MATSUMOTO, Melissa3 ; VATTAY, Anthony3 ; MANIARA, Wieslawa4 ; AMARAL, Adam4 ; DORSCH, Marion3 ; KELLEHER, Joseph F2 ; MCEWAN, Michael A1 ; KARKI, Rajesh1 ; LLAMAS, Luis1 ; YUSUFF, Naeem1 ; FENG HE1 ; YANHONG LI1 ; YINGCHUAN SUN1
[1] Department of Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 01239, United States
[2] Department of Developmental and Molecular Pathways, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 01239, United States
[3] Department of Oncology, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 01239, United States
[4] Department of Metabolism and Pharmacokinetics, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 01239, United States - Source
Journal of medicinal chemistry (Print). 2009, Vol 52, Num 13, pp 3954-3968, 15 p ; ref : 29 ref
- CODEN
- JMCMAR
- ISSN
- 0022-2623
- Scientific domain
- Pharmacology drugs
- Publisher
- American Chemical Society, Columbus, OH
- Publication country
- United States
- Document type
- Article
- Language
- English
- Keyword (fr)
- Animal Antagoniste Anticancéreux Biodisponibilité Cellule tumorale Dérivé de la phtalazine Dérivé de la pipérazine Dérivé de la pyridine Encéphale In vitro In vivo Molécule petite Médulloblastome Pharmacocinétique Relation structure activité Récepteur couplé protéine G Souris Synthèse chimique Système nerveux central Transduction signal Voie intraveineuse Voie orale Voie de signalisation Hedgehog Mammalia Rodentia Vertebrata
- Keyword (en)
- Animal Antagonist Antineoplastic agent Bioavailability Tumor cell Phthalazine derivatives Piperazine derivatives Pyridine derivatives Encephalon In vitro In vivo Small molecule Medulloblastoma Pharmacokinetics Structure activity relation G protein coupled receptor Mouse Chemical synthesis Central nervous system Signal transduction Intravenous administration Oral administration Hedgehog signaling pathway Mammalia Rodentia Vertebrata
- Keyword (es)
- Animal Antagonista Anticanceroso Biodisponibilidad Célula tumoral Piperazina derivado Piridina derivado Encéfalo In vitro In vivo Molécula pequeña Meduloblastoma Farmacocinética Relación estructura actividad Receptor acoplado proteína G Ratón Síntesis química Sistema nervioso central Transducción señal Vía intravenosa Vía oral Mammalia Rodentia Vertebrata
- 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
- 22092586
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/jm900309j 
https://dx.doi.org/10.1021/jm900309j
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