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Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists

Author
RABOISSON, Pierre; MARUGAN, Juan José; LATTANZE, Jennifer; PARKS, Daniel J; CUMMINGS, Maxwell D; SCHUBERT, Carsten; KOBLISH, Holly K; TIANBAO LU; SHUYUAN ZHAO; PLAYER, Mark R; MARONEY, Anna C; REED, Rolanda L; HUEBERT, Norman D
Departments of Medicinal Chemistry, Structural Biology and Molecular Design and Informatics, Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 665 Stockton Drive, Exton, PA 19341, United States
Source

Bioorganic & medicinal chemistry letters (Print). 2005, Vol 15, Num 7, pp 1857-1861, 5 p

ISSN
0960-894X
Scientific domain
Biochemistry, molecular biology, biophysics; Pharmacology drugs
Publisher
Elsevier, Oxford
Publication country
United Kingdom
Document type
Article
Language
English
Keyword (fr)
Antagoniste Anticancéreux Benzène dérivé Composé non peptide Composé peptidomimétique Cycle 7 chaînons Côlon Fixation biologique Gène TP53 Gène onc Gène suppresseur tumeur Homme Hétérocycle azote In vitro Inhibition Interaction moléculaire Intestin Lactame Lignée cellulaire Modèle moléculaire Modélisation Perméabilité cellulaire Produit gène Relation structure activité Synthèse chimique Transduction signal 1,4-Diazépine-1-valérique acide(3-[4-chlorophényl]-4-[1-(4-chlorophényl)éthyl]-2,5-dioxo-7-phényl-1,2,3,4-tétrahydro) 1,4-Diazépine-1-valérique acide(7-[4-bromophényl]-3-[4-chlorophényl]-4-[1-(4-chlorophényl)éthyl]-2,5-dioxo-1,2,3,4-tétrahydro) Gène hdm2 Lignée CACO2 Brome Composé organique Chlore Composé organique
Keyword (en)
Antagonist Antineoplastic agent Benzene derivatives Non peptide compound Peptidomimetic compound Seven membered ring Colon Biological fixation TP53 Gene Onc gene Tumor suppressor gene Human Nitrogen heterocycle In vitro Inhibition Molecular interaction Gut Lactam Cell line Molecular model Modeling Cell permeability Gene product Structure activity relation Chemical synthesis Signal transduction Bromine Organic compounds Chlorine Organic compounds
Keyword (es)
Antagonista Anticanceroso Benceno derivado Compuesto no péptido Compuesto peptidomimético Ciclo 7 eslabones Colón Fijación biológica Gen TP53 Gen onc Gen supresor tumor Hombre Heterociclo nitrógeno In vitro Inhibición Interacción molecular Intestino Lactamo Línea celular Modelo molecular Modelización Permeabilidad celular Producto gene Relación estructura actividad Síntesis química Transducción señal Bromo Compuesto orgánico Cloro Compuesto orgánico
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
16626927

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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