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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / therapeutic use
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Benzazepines / chemical synthesis
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Benzazepines / therapeutic use
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Carbamates / chemical synthesis*
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Carbamates / therapeutic use
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Isoquinolines / chemical synthesis
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Isoquinolines / therapeutic use
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Leukemia P388 / drug therapy*
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Leukemia, Experimental / drug therapy*
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Mice
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Pyrroles / chemical synthesis
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Pyrroles / therapeutic use
Substances
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Antineoplastic Agents
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Benzazepines
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Carbamates
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Isoquinolines
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Pyrroles