Abstract
Pictet-Spengler condensation of aldehydes or alpha-keto-esters with 4-(2-anilinophenyl)-7-azaindole (11) or deazapurine (12) gave high yields of the 3,4-fused cyclic compounds. SAR studies, by varying the substituted benzaldehyde components, lead to the discovery of a series of potent JAK2 kinase inhibitors.
Copyright 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Benzaldehydes / chemistry
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Binding Sites
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Cell Line
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Crystallography, X-Ray
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Drug Discovery
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Humans
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Indoles / chemistry*
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Janus Kinase 2 / antagonists & inhibitors*
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Janus Kinase 2 / metabolism
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacology
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Purines / chemistry*
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Structure-Activity Relationship
Substances
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7-azaindole dimer
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Benzaldehydes
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Indoles
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Protein Kinase Inhibitors
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Purines
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Janus Kinase 2
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benzaldehyde