Synthesis and Cytotoxic Activity of Acronycine Derivatives Modified at the Pyran Ring

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概要

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• Nitration of acronycine (1) and 6-demethoxyacronycine (3) afforded 2-nitroacronycine (2) and 2-nitro-6-demethoxyacronycine (4), respectively. Reduction of 2-nitroacronycine yielded, depending on the conditions, 2-nitro-1,2-dihydroacronycine (5), 2-oxo-1,2-dihydroacronycine oxime (7) or 2-amino-1,2-dihydroacronycine (6). This latter was readily converted into 2-dimethylamino-1,2-dihydroacronycine (8), 2-acetylamino-1,2-dihydro-acronycine (9) and 2-benzoylamino-1,2-dihydroacronycine (10).The cytotoxicity of these compounds was evaluated against L1210 leukemia cells. Compounds 2 and 7 were 300- and 10-fold more potent than acronycine in inhibiting L1210 cell proliferation, respectively. Compound 2 was devoid of antitumor activity against P388 leukemia and C38 colon adenocarcinoma.

• 公益社団法人日本薬学会の論文
• 1996-11-15

著者

• Koch Michel

  Laboratoire De Pharmacognosie De I'universite Rene Descartes U.m.r. C.n.r.s. N° 8638 Faculte De

• Michel Sylvie

  Laboratoire De Pharmacognosie De I'universite Rene Descartes U.m.r. C.n.r.s. N° 8638 Faculte De

• Koch M

  Univ. Rene Descartes Paris Fra

• TILLEQUIN Francois

  Laboratoire de Pharmacognosie de l'Universite Paris Descartes

• PIERRE Alain

  Institut de Recherches Servier, Division Recherche Cancerologie

• SKALTSOUNIS Alexios-Leandros

  University of Athens, Department of Pharmacy, Division of Pharmacognosy

• ATASSI Ghanem

  Institut de Recherches "SERVIER"

• ROLLAND Yves

  Institut de Recherches Servier, Division de Cancerologie Experimentale

• ELOMRI Abdelhakim

  Laboratoire de Pharmacognosie de l'Universite de Rouen-Haute Normandie

• SKALTSOUNIS Alexios-Leandros

  Laboratory of Pharmacognosy, University of Athens

• Pierre Alain

  Institut De Recherches Servier Division Recherche Cancerologie

• Mitaku S

  Laboratory Of Pharmacognosy Department Of Pharmacy University Of Athens

• Rolland Yves

  Institut De Recherche Servier

• Atassi G

  Inst. Res. Servier Suresnes Fra

• Elomri Abdelhakim

  Laboratoire De Pharmacognosie De L'universite De Rouen-haute Normandie Umr 6014 Cnrs Faculte De

• Tillequin Francois

  Laboratoire De Pharmacognosie De L'universite Paris Descartes

• Tillequin F

  Laboratoire De Pharmacognoise De 1'universite Rene Descartes Umr/cnrsn ^○8638 Faculte Des Scien

• Mitaku Sofia

  Laboratory Of Pharmacognosy Department Of Pharmacy University Of Athens

• Skaltsounis A‐l

  University Of Athens Department Of Pharmacy Division Of Pharmacognosy

• Skaltsounis Alexios-leandros

  Laboratory Of Pharmacognosy Department Of Pharmacy University Of Athens

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