Synthesis of New Aromatic Pyrrolo[2,1- c] [1,4]benzodiazepines and Pyrrolo[1,2- a] thieno[3,2- e] [1,4]diazepines as Anti-tumoral Agents |
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| Authors: | Vincent Lisowski Frédéric Fabis Alain Pierré Daniel-Henri Caignard Pierre Renard Sylvain Rault |
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| Affiliation: | 1. Centre d'Etudes et de Recherche sur le Médicament de Normandie-UFR des Sciences Pharmaceutiques 5, rue Vaubénard 14032 Caen cedex, France;2. ADIR, 1 rue Carle Hébert 92415 Courbevoie Cedex, France |
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| Abstract: | Diazepine analogs of thieno[2,3- b] pyrrolizin-8-ones were synthesized by aromatization of 2-hydroxypyrrolo[1,2- a] thieno[3,2- e] [1,4]diazepines. These compounds were evaluated in vitro for their antiproliferative activity against the L1210 leukemia cell line. The activity of these compounds was in the micromolar range, the best result being for the mixture of the isomers 5 and 6 which showed a 0.35 μM IC 50 against cell growth. |
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| Keywords: | Thieno[2,3- b] pyrrolizin-8-ones Pyrrolo[1,2- a] thieno [3,2- e] [1,4]diazepines Aromatization Antiproliferative Leukemia |
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