Abstract
Cyanoguanidine derivatives of loratadine (3a-i) were synthesized and screened for antitumor and anti-inflammatory activity. The most promising compound 3c (R=n-C(8)H(17)) possessed at least twofold higher in vitro cytotoxicity than 5-fluorouracil against mammary (MCF-7 and MDA-MB 231) as well as colon (HT-29) carcinoma cells. The mode of action, however, is so far unclear. The participation of the COX-1/2 enzymes on the cytotoxicity, however, is very unlikely. Nevertheless all compounds showed stronger in vivo anti-inflammatory activity than ibuprofen in the xylene-induced ear swelling assay in mice.
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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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / 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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Cell Line, Tumor
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Cell Proliferation / drug effects
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Ear Diseases / chemically induced
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Ear Diseases / drug therapy*
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Guanidines / chemistry*
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HT29 Cells
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Humans
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Loratadine / analogs & derivatives*
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Loratadine / chemistry
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Loratadine / pharmacology*
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MCF-7 Cells
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Male
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Mice
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Mice, Inbred Strains
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Molecular Structure
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Structure-Activity Relationship
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Xylenes
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Antineoplastic Agents
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Guanidines
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Xylenes
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Loratadine
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dicyandiamido