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Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis

Author
IOANOVICIU, Alexandra1 ; ANTONY, Smitha2 ; POMMIER, Yves2 ; STAKER, Bart L3 ; STEWART, Lance3 ; CUSHMAN, Mark1
[1] Department of Medicinal Chemistry and Molecular Pharmacology and the Purdue Cancer Center, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907, United States
[2] Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland 20892-4255, United States
[3] deCODE biostructures, Inc., 7869 Northeast Day Road West, Bainbridge Island, Washington 98110, United States
Source

Journal of medicinal chemistry (Print). 2005, Vol 48, Num 15, pp 4803-4814, 12 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)
Anticancéreux Cellule tumorale Complexe enzyme inhibiteur Composé aromatique Composé pentacyclique Composé polycyclique Cytotoxicité DNA topoisomerase Diffraction RX Hétérocycle azote Hétérocycle oxygène azote In vitro Inhibiteur enzyme Lignée cellulaire Modèle moléculaire Modèle électrostatique Mécanisme action Relation structure activité Structure cristalline Synthèse chimique Indéno[1,2-c]isoquinoléine dérivé Indénoisoquinoléine Enzyme Isomerases
Keyword (en)
Antineoplastic agent Tumor cell Inhibitor enzyme complex Aromatic compound Pentacyclic compound Polycyclic compound Cytotoxicity DNA topoisomerase X ray diffraction Nitrogen heterocycle Oxygen nitrogen heterocycle In vitro Enzyme inhibitor Cell line Molecular model Electrostatic model Mechanism of action Structure activity relation Crystalline structure Chemical synthesis Enzyme Isomerases
Keyword (es)
Anticanceroso Célula tumoral Complejo enzima inhibidor Compuesto aromático Compuesto pentacíclico Compuesto policíclico Citotoxicidad DNA topoisomerase Difracción RX Heterociclo nitrógeno Heterociclo oxígeno nitrógeno In vitro Inhibidor enzima Línea celular Modelo molecular Modelo electrostático Mecanismo acción Relación estructura actividad Estructura cristalina Síntesis química Enzima Isomerases
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
16989178

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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