Synthesis and antiproliferative evaluation of 7-aminosubstituted pyrroloiminoquinone derivatives

Coupling of five amines on the 7-methoxy-1,3,4,5-tetrahydropyrrolo[4,3,2- de]quinoline core was achieved and afforded, in particular, an opened analogue of the natural alkaloid wakayin. Evaluation of cytotoxic activity of compounds 2, 10– 13 on L1210 cells afforded IC 50 in the range 0.25–5.3 μM....

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Published in:Bioorganic & medicinal chemistry letters 2000-10, Vol.10 (19), p.2231-2234
Main Authors: Bénéteau, Valérie, Pierré, Alain, Pfeiffer, Bruno, Renard, Pierre, Besson, Thierry
Format: Article
Language:English
Subjects:
Alkaloids - chemistry
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
General aspects
Leukemia L1210
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Pyrroles - chemical synthesis
Pyrroles - chemistry
Pyrroles - pharmacology
Quinolones - chemical synthesis
Quinolones - chemistry
Quinolones - pharmacology
Rats
Tumor Cells, Cultured
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Summary:Coupling of five amines on the 7-methoxy-1,3,4,5-tetrahydropyrrolo[4,3,2- de]quinoline core was achieved and afforded, in particular, an opened analogue of the natural alkaloid wakayin. Evaluation of cytotoxic activity of compounds 2, 10– 13 on L1210 cells afforded IC 50 in the range 0.25–5.3 μM.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00450-9