Abstract
A series of C-H functionalisation plate-based chemical screens and other C-H activation protocols were developed for the chemical diversification of drug molecules. In this Letter, metalloporphyrin and other catalytic oxidation systems are described in addition to chlorination. Mifepristone and antalarmin are used as substrates. The products obtained and the biological data demonstrate the potential utility of this approach.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Biomimetics
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Carbon / chemistry
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Chemistry, Pharmaceutical / methods*
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Chlorine / chemistry
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Drug Design
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Humans
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Hydrogen / chemistry
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Inhibitory Concentration 50
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Metalloporphyrins / chemistry
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Metals / chemistry
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Microsomes, Liver / drug effects
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Mifepristone / pharmacology*
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Models, Chemical
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Oxygen / chemistry
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Pyrimidines / pharmacology*
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Pyrroles / pharmacology*
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Structure-Activity Relationship
Substances
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Metalloporphyrins
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Metals
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Pyrimidines
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Pyrroles
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antalarmin
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Mifepristone
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Chlorine
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Carbon
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Hydrogen
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Oxygen