Abstract
We report an improved single-step synthesis to generate the membrane-permeant acetoxymethyl esters (AM-esters) of cGMP and three cGMP-analogues. These bioactivatable compounds were found to induce cell death in rat IPC-81 cells, a model system for acute myelocytic leukemia, in micromolar doses, while the corresponding non-modified cGMP-analogues were inactive.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology
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Biotransformation
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Cell Death / drug effects
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Cell Line
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Cell Membrane Permeability / drug effects
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Cyclic GMP / analogs & derivatives*
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Cyclic GMP / chemical synthesis
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Cyclic GMP / pharmacology
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Humans
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Leukemia, Experimental / drug therapy*
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Leukemia, Myeloid, Acute / drug therapy
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Rats
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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8-bromocyclic GMP
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Cyclic GMP