Abstract
Aided by Structure Based Drug Discovery (SBDD), we rapidly designed a highly novel and selective series of mTOR inhibitors. This chemotype conveys exquisite kinase selectivity, excellent in vitro and in vivo potencies and ADME safety profiles. These compounds could serve as good tools to explore the potential of TORC inhibition in various human diseases.
Keywords:
Inhibitor; SBDD; mTOR.
Copyright © 2019 Elsevier Ltd. All rights reserved.
MeSH terms
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Binding, Competitive
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Drug Discovery
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Furans / chemistry*
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Humans
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Models, Molecular
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Molecular Structure
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Morpholines / chemistry
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Phosphatidylinositol 3-Kinase / chemistry
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Protein Binding
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / metabolism*
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Pyridines / chemistry*
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Pyrimidines / chemistry*
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Structure-Activity Relationship
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TOR Serine-Threonine Kinases / antagonists & inhibitors*
Substances
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Furans
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Morpholines
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PI103
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Protein Kinase Inhibitors
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Pyridines
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Pyrimidines
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morpholine
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Phosphatidylinositol 3-Kinase
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TOR Serine-Threonine Kinases
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pyrimidine