Abstract
In an effort to generate novel anticancer agents, a series of hybrids of alpha-methylene-gamma-lactones and 2-phenyl indoles has been synthesized and evaluated for inhibition activities on the phosphorylation of AKT, mTOR, p70S6 kinase, and 4E-BP1. The results indicate that substitutes on the gamma-position of lactones have a rather significant influence on inhibition activities.
MeSH terms
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Adaptor Proteins, Signal Transducing
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Carrier Proteins / drug effects
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Carrier Proteins / metabolism
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Cell Cycle Proteins
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Humans
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Lactones / chemical synthesis*
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Lactones / pharmacology
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Phosphoproteins / drug effects
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Phosphoproteins / metabolism
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Phosphorylation / drug effects
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / pharmacology
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Protein Kinases / drug effects*
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Protein Kinases / metabolism
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Ribosomal Protein S6 Kinases, 70-kDa / drug effects
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Ribosomal Protein S6 Kinases, 70-kDa / metabolism
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Signal Transduction / drug effects
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Structure-Activity Relationship
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TOR Serine-Threonine Kinases
Substances
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Adaptor Proteins, Signal Transducing
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Antineoplastic Agents
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Carrier Proteins
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Cell Cycle Proteins
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EIF4EBP1 protein, human
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Indoles
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Lactones
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Phosphoproteins
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Protein Kinase Inhibitors
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Protein Kinases
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MTOR protein, human
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Ribosomal Protein S6 Kinases, 70-kDa
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TOR Serine-Threonine Kinases