Synthesis and Biological Evaluation of Monoindolyl and Indolocarbazolyl Oxazolones and Imidazolones

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概要

• 論文の詳細を見る

• Eight compounds structurally related to protein kinase C inhibitor MDL 27032 and substituted with indole moieties were synthesized. Their activities towards protein kinase C (PKC) and protein kinase A (PKA) were determined. Their effect on PKC-mediated contraction of rat tracheal smooth muscle, their antiproliferative activity on two murine tumor cell lines, melanoma B16 and leukemia P388 and their antimicrobial activity on a gram-positive bacterium Bacillus cereus were also examined. The mammalian and bacterial cell antiproliferative activity, as well as vasorelaxant effect, observed for some of them could not be correlated to PKC or PKA inhibition. Only bulky bis-indolyl compounds exhibited biological activity in these experiments. Rigid indolocarbazoles had the strongest antiproliferative activity.

• 公益社団法人日本薬学会の論文
• 1997-04-15

著者

• Sancelme Martine

  Universite Blaise Pascal Laboratoire De Chimie Organique Biologique

• Sancelme Martine

  Universite Blaise Pascal Synthese Electrosynthese Et Etude De Systemes A Interet Biologique

• Meyer Thomas

  Department Of Cardiology University Of Marburg

• Meyer Thomas

  Departement D'oncologie

• RODRIGUES PEREIRA

  Universite Blaise Pascal, Synthese, Electrosynthese et Etude de Systemes a Interet Biologique

• PRUDHOMME Michelle

  Universite Blaise Pascal, Synthese, Electrosynthese et Etude de Systemes a Interet Biologique

• OLLIER Monique

  Unite INSERM U71

• CREVEL Henri

  Laboratoire de Physiologie, Universite Bordeaux II

• SAVINEAU Jean

  Laboratoire de Physiologie, Universite Bordeaux II

• FABBRO Doriano

  Departement d'Oncologie

• Crevel Henri

  Laboratoire De Physiologie Universite Bordeaux Ii

• Savineau Jean

  Laboratoire De Physiologie Universite Bordeaux Ii

• Fabbro Doriano

  Departement D'oncologie

• Rodrigues Pereira

  Universite Blaise Pascal Synthese Electrosynthese Et Etude De Systemes A Interet Biologique

• Prudhomme Michelle

  Universite Blaise Pascal Synthese Electrosynthese Et Etude De Systemes A Interet Biologique

関連論文

• Ultrastructural Alterations in Acquired Aortic and Mitral Valve Disease as Revealed by Scanning and Transmission Electron Microscopical Investigations
• Synthesis and Biological Evaluation of Monoindolyl and Indolocarbazolyl Oxazolones and Imidazolones
• Activated STAT1 and STAT5 transcription factors in extramedullary hematopoietic tissue in a polycythemia vera patient carrying the JAK2 V617F mutation
• Confusion by Frequent Changes in Staging of Exocrine Pancreatic Carcinoma
• Syntheses and Antimicrobial Activities of Five-membered Ring Heterocycles Coupled to Indole Moieties
• Antimicrobial Activities of Indolocarbazole and Bis-indole Protein Kinase C Inhibitors II.Substitution on Maleimide Nitrogen with Functional Groups Bearing a Labile Hydrogen

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