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CONCEPTION, SYNTHESE ET EVALUATION PHARMACOLOGIQUE DE γ-CARBOLINES, INHIBITEURS POTENTIELS DE 5-LIPOXYGENASE ET DE CYCLOOXYGENASES.

Alexandre Bridoux-2005-01-01-HAL (Le Centre pour la Communication Scientifique Directe)
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TL;DRAbstract

Two key enzymatic systems in the inflammation process revealed being implicated <br />in many cancers (colon, pancreas, breast, lung) and more particularly in prostate cancer (PCa). The 5-lipoxygenase (5-LO) monitors leucotrienes' formation which are inflammation of allergy mediators. There are two isoforms of the cyclooxygenase enzyme : COX1 and COX2. COX1 <br />is constitutively expressed and COX2 is the inducible isoform. The cyclooxygenases monitor <br />the formation of the prostaglandins, responsive inflammation mediators. Facing the similarities of the overexpressions of those enzymes in human cancer, a new treatment based on <br />the disregulation of the arachidonic acid metabolism can be considered. The purpose of this study is to participate to the PCa therapeutical research particularly in its hormono-independant state by the rational design, the organic synthesis and then the pharmacological valuation of some <br />N-benzoyltetrahydro-γ-carbolines, a new class of potential

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Two key enzymatic systems in the inflammation process revealed being implicated <br />in many cancers (colon, pancreas, breast, lung) and more particularly in prostate cancer (PCa). The 5-lipoxygenase (5-LO) monitors leucotrienes' formation which are inflammation of allergy mediators. There are two isoforms of the cyclooxygenase enzyme : COX1 and COX2. COX1 <br />is constitutively expressed and COX2 is the inducible isoform. The cyclooxygenases monitor <br />the formation of the prostaglandins, responsive inflammation mediators. Facing the similarities of the overexpressions of those enzymes in human cancer, a new treatment based on <br />the disregulation of the arachidonic acid metabolism can be considered. The purpose of this study is to participate to the PCa therapeutical research particularly in its hormono-independant state by the rational design, the organic synthesis and then the pharmacological valuation of some <br />N-benzoyltetrahydro-γ-carbolines, a new class of potential

Keywords

ChemistryMolecular biologyBiology

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