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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2002-1-24
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pubmed:abstractText |
Heterocyclic phenazinecarboxamides were prepared by condensation of aminoheterocycles and 2-halo-3-nitrobenzoic acids, followed by reductive ring closure and amidation. They showed similar inhibition of paired cell lines that underexpressed topo II or overexpressed P-glycoprotein, indicating a non topo II mechanism of cytotoxicity and indifference to P-glycoprotein mediated multidrug resistance. Compounds with a fused five-membered heterocyclic ring were generally less potent than the pyrido[4,3-a]phenazines. A 4-methoxypyrido[4,3-a]phenazine (IC(50)s 2.5-26 nM) gave modest (ca. 5 day) growth delays in H69/P xenografts with oral dosing.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
31
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
740-3
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:11806725-Amides,
pubmed-meshheading:11806725-Animals,
pubmed-meshheading:11806725-Antineoplastic Agents,
pubmed-meshheading:11806725-Drug Resistance, Multiple,
pubmed-meshheading:11806725-Drug Resistance, Neoplasm,
pubmed-meshheading:11806725-Drug Screening Assays, Antitumor,
pubmed-meshheading:11806725-Enzyme Inhibitors,
pubmed-meshheading:11806725-Heterocyclic Compounds with 4 or More Rings,
pubmed-meshheading:11806725-Humans,
pubmed-meshheading:11806725-Intercalating Agents,
pubmed-meshheading:11806725-Mice,
pubmed-meshheading:11806725-Neoplasm Transplantation,
pubmed-meshheading:11806725-P-Glycoprotein,
pubmed-meshheading:11806725-Phenazines,
pubmed-meshheading:11806725-Structure-Activity Relationship,
pubmed-meshheading:11806725-Topoisomerase II Inhibitors,
pubmed-meshheading:11806725-Transplantation, Heterologous,
pubmed-meshheading:11806725-Tumor Cells, Cultured
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pubmed:year |
2002
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pubmed:articleTitle |
Structure-activity relationships for pyrido-, imidazo-, pyrazolo-, pyrazino-, and pyrrolophenazinecarboxamides as topoisomerase-targeted anticancer agents.
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pubmed:affiliation |
Auckland Cancer Society Research Centre, Faculty of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland, New Zealand.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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