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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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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

Vincent Lisowski, Frédéric Fabis, Alain Pierré, Daniel-Henri Caignard, Pierre Renard et Sylvain Rault
Journal of enzyme inhibition and medicinal chemistry, Vol.17(6), pp.403-407
01/01/2002
DOI: https://doi.org/10.1080/1475636021000005712
PMID: 12683676

Résumé

Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Benzene Derivatives - chemistry Benzodiazepines - chemistry Benzodiazepines - pharmacology Cell Division - drug effects Drug Screening Assays, Antitumor Inhibitory Concentration 50 Isomerism Leukemia L1210 - drug therapy Mice Structure-Activity Relationship Tumor Cells, Cultured
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 microM IC50 against cell growth.

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