Abstract
Exploration for new MDR-modulator utilizing tetrahydroisoquinoline as scaffold disclosed 6,7-dimethoxy-1-(3,4-dimethoxy)benzyl-2-(N-n-octyl-N'-cyano)guanyl-1,2,3,4-tetrahydroisoquinoline (7) as a readily accessible medicinal lead. Compound 7 possessed potent MDR reversal activity in the range of the reference compound verapamil, and had not cardiovascular activity compared to verapamil.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amidines* / chemical synthesis
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Amidines* / chemistry
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Amidines* / pharmacology
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Animals
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Anti-Arrhythmia Agents / chemical synthesis
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Anti-Arrhythmia Agents / chemistry
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Anti-Arrhythmia Agents / pharmacology
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Antineoplastic Agents* / chemical synthesis
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Antineoplastic Agents* / chemistry
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Antineoplastic Agents* / pharmacology
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Arrhythmias, Cardiac / drug therapy
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Dose-Response Relationship, Drug
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Drug Design
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Drug Resistance, Multiple / drug effects*
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Drug Resistance, Neoplasm / drug effects*
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Drug Screening Assays, Antitumor
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Humans
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Isoquinolines* / chemical synthesis
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Isoquinolines* / chemistry
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Isoquinolines* / pharmacology
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Mice
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Mice, Nude
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Myocardial Contraction / drug effects
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Neoplasms / drug therapy*
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Neoplasms / pathology
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
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Tetrahydroisoquinolines* / chemical synthesis
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Tetrahydroisoquinolines* / chemistry
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Tetrahydroisoquinolines* / pharmacology
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Time Factors
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Verapamil / adverse effects
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Verapamil / pharmacology
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Verapamil / therapeutic use
Substances
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6,7-dimethoxy-1-(3,4-dimethoxy)benzyl-2-(N-n-octyl-N'-cyano)guanyl-1,2,3,4-tetrahydroisoquinoline
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Amidines
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Anti-Arrhythmia Agents
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Antineoplastic Agents
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Isoquinolines
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Tetrahydroisoquinolines
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Verapamil