Abstract
A novel series of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor is reported. Starting from a 3.4 microM high throughput screen hit, members of this series have been identified which are full agonists with functional potency <50 nM and oral bioavailability in mice.
MeSH terms
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Administration, Oral
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Animals
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Benzene Derivatives / chemical synthesis*
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Benzene Derivatives / chemistry
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Benzene Derivatives / pharmacology*
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Carbazoles / chemical synthesis*
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Carbazoles / chemistry
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Carbazoles / pharmacology*
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Combinatorial Chemistry Techniques
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Drug Design
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Humans
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Mice
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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Receptors, Thrombopoietin / agonists*
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Receptors, Thrombopoietin / chemistry
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Structure-Activity Relationship
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Thrombopoietin* / chemistry
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Thrombopoietin* / metabolism
Substances
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Benzene Derivatives
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Carbazoles
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Receptors, Thrombopoietin
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Thrombopoietin