Abstract
Five novel acetogenin analogues with a furan, thiophene, or thiazole ring were synthesized, and their inhibitory activities toward human cancer cell lines were evaluated. The analogues showed more potent activities than natural acetogenin. One of them, the thiophene-3-carboxamide analogue, strongly inhibited the growth of human lung cancer cell line NCI-H23 in the xenograft mouse assay without critical toxicity.
Keywords:
Annonaceous acetogenin; Antitumor activity; Chemical synthesis; Structure–activity relationship.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetogenins / chemical synthesis
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Acetogenins / chemistry
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Acetogenins / pharmacology*
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Amides / administration & dosage
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Amides / chemistry
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Amides / pharmacology*
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Animals
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Antineoplastic Agents / administration & dosage
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Female
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Humans
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Mice
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Mice, Inbred BALB C
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Mice, Nude
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Molecular Structure
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Neoplasms, Experimental / drug therapy*
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Neoplasms, Experimental / pathology
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Structure-Activity Relationship
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Thiophenes / administration & dosage
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Thiophenes / chemistry
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Thiophenes / pharmacology*
Substances
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Acetogenins
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Amides
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Antineoplastic Agents
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Thiophenes