Abstract
Novel series of N-benzyl 1,4-dihydropyridines have been prepared by facile syntheses. All relevant substituents of the molecular scaffold have been varied. The resulting compounds were biologically evaluated as P-glycoprotein (P-gp) inhibitors. Substitutions of the N-benzyl residue favour biological activity beside respective 3-ester functions. Most active compounds were further evaluated as multidrug resistance (MDR) modulators to restore the cytotoxic properties of varying daunorubicin applications.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Animals
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Antibiotics, Antineoplastic / pharmacology
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Cell Line, Tumor
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Cell Survival / drug effects
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Daunorubicin / pharmacology
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Dihydropyridines / chemistry*
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Dihydropyridines / pharmacology*
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Drug Resistance, Multiple / drug effects*
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Drug Resistance, Neoplasm / drug effects
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Humans
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Mice
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Neoplasms / drug therapy
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Neoplasms / metabolism
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Structure-Activity Relationship
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Antibiotics, Antineoplastic
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Dihydropyridines
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1,4-dihydropyridine
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Daunorubicin