Abstract
The known DNMT inhibitor SGI-1027 4 has been synthesized using as key steps Pd-catalyzed Ar-N bond formation reactions performed in a sequential or convergent manner. In the former approach, a by-product, which corresponds to the incorporation of two units of 4-chloroquinoline, was also isolated. The biological effects of compound 4 in the U937 human leukemia cell line are also described.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminoquinolines / chemical synthesis
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Aminoquinolines / chemistry*
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Aminoquinolines / pharmacology
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Catalysis
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Cell Cycle Checkpoints / drug effects
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DNA (Cytosine-5-)-Methyltransferases / antagonists & inhibitors*
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DNA (Cytosine-5-)-Methyltransferases / metabolism
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Humans
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Leukemia / enzymology
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Leukemia / pathology
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Palladium / chemistry
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology
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U937 Cells
Substances
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Aminoquinolines
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Enzyme Inhibitors
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Pyrimidines
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SGI-1027
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Palladium
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DNA (Cytosine-5-)-Methyltransferases