Synthesis of Mannich Bases of 5-Hydroxynaphthalene-1,8-carbolactone as Potential Antifungal or Antitumor Agents

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概要

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• Mannich bases of 5-hydroxynaphthalene-1,8-carbolactone 1 were prepared from various secondary amines or bulky primary amines and formaldehyde.They were isolated in almost all cases as hydrochlorides. These derivatives were submitted to in vitro antifungal and cytotoxic assays. The antifungal assays were performed against three strains of yeasts and five strains of human pathogenic fungi. Two of the tested compounds, 2i and 2j, exhibited interesting antifungal activities against Candida albicans and Candida tropicalis. The cytotoxic activity was evaluated towards L 1210 leukemia cells. Almost all of the Mannich bases had shown significant activity against this tumor cell line as values of IC_<50> ⩽4 μg/ml are considered interesting. Only one derivative 2 developed better cytotoxicity than the parent compound 1.

• 公益社団法人日本薬学会の論文
• 1991-02-25

著者

• Fillion H

  Univ. Claude Bernard Lyon I Lyon Cedex Fra

• Fillion Houda

  Laboratoire De Chimie Organique Faculte De Pharmacie Universite Claude Bernard Lyon

• Fillion Houda

  Laboratoire De Chimie Organique

• BOUAZIZ Zouhair

  Laboratoire de Chimie Organique

• Bouaziz Z

  Laboratoire De Chimie Organique Institut Des Sciences Pharmaceutiques Et Biologiques Universite Clau

• BERLION Maryse

  Laboratoire de Physiologie et Pharmacologie I, Faculte de Pharmacie de Grenoble

• BARTOLI Marie-Helene

  Laboratoire de Biotechnique et de Pharmacie Clinique GREPO, UFR de Pharmacie de Grenoble, Universite

• PORTE Monique

  Laboratoire de Mycologie

• VILLARD Jean

  Laboratoire de Mycologie

• Berlion Maryse

  Laboratoire De Biotechnique Et De Pharmacie Clinique Grepo Ufr De Pharmacie De Grenoble Universite J

• Berlion Maryse

  Laboratoire De Physiologie Et Pharmacologie I

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• Diels-Alder Reactions between Dienamides and Quinones : Stereochemistry of the Cycloadditions and Cytotoxic Activity of the Adducts
• Generation of a Thiazole o-Quinodimethane from an Imino Derivative and Its Intermolecular Diels-Alder Trapping with Alkynes or Quinones
• Studies on the Oxidative Addition of N, N-Dimethylamine to Bromojuglones and Bromomethyljuglones
• HETERO DIELS-ALDER REACTION WITH INDOLOQUINONES
• Synthesis of Furnaphth[1,3]oxazine and Furo[1,3]oxazinoquinoline Derivatives as Precursors for an o-Quinonemethide Structure and Potential Antitumor Agents
• Synthesis of Mannich Bases of 5-Hydroxynaphthalene-1,8-carbolactone as Potential Antifungal or Antitumor Agents
• Synthesis and Diels-Alder Reactivity of ortho-Carbazolequinones
• Reactivity of an o-Indoloquinone to 1-and 2-Azadienes

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