Abstract
Three new 5'-O-acyl tiazofurin derivatives 2-4 were synthesized and evaluated for their antiproliferative activity against different tumour cell lines as well as for their ability to induce apoptosis in C6 cells in vitro. Apart of the antitumour assays, the cell membrane permeation of 2-4 and their intracellular metabolism in C6 cells in vitro was also studied in order to evaluate their potential as possible tiazofurin bioisosteres or prodrugs.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects
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Cell Division / drug effects
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Cell Line, Tumor
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Cell Survival / drug effects
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Chemical Phenomena
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Chemistry, Physical
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DNA, Neoplasm / biosynthesis
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DNA, Neoplasm / genetics
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Drug Screening Assays, Antitumor
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Humans
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In Situ Nick-End Labeling
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Mice
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Ribavirin / analogs & derivatives*
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Ribavirin / chemical synthesis
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Ribavirin / pharmacology
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Spectrophotometry, Infrared
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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DNA, Neoplasm
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Indicators and Reagents
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Ribavirin
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tiazofurin