Paper
Synthesis and antileukemic activity of bis[[(carbamoyl)oxy]methyl]- substituted pyrrolo[2,1-a]isoquinolines, pyrrolo[1,2-a]quinolines, pyrrolo[2,1-a]isobenzazepines, and pyrrolo[1,2-a]benzazepines.
Published Nov 1, 1988 · W. Anderson, A. R. Heider, N. Raju
Journal of medicinal chemistry
79
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Abstract
A series of bis[[(carbamoyl)oxy]methyl]-substituted pyrrole-fused tricyclic heterocycles were synthesized by using 1,3-dipolar cycloaddition reactions with a trifluoromethanesulfonate salt of an appropriate Resissert compound or with a mesoionic oxazolone intermediate. All of the bis(carbamates) were active in vivo against P388 lymphocytic leukemia with 5,6-dihydro-8-methoxy-1,2- bis(hydroxymethyl)pyrrolo[2,1-a]isoquinoline bis[N-(2-propyl)carbamate] (3c) showing the highest level of activity.
Bis[[(carbamoyl)oxy]methyl]-substituted pyrrole-fused tricyclic heterocycles show antileukemic activity against P388 lymphocytic leukemia, with 5,6-dihydro-8-methoxy-1,2-
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