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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
1987-9-24
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pubmed:abstractText |
(-)-Indolactam-V, which has the partial structure of teleocidins A and B, and has tumor-promoting activity, is a good model for use in studies on the relation between structure and tumor-promoting activity, whereas (+)-indolactam-V has no tumor-promoting activity. In this work, five racemic indolactams differing only in their alkyl group at C-12 of (-)-indolactam-V were synthesized and tested for biological and biochemical activities related to tumor promotion. The activities tested were inductions of ornithine decarboxylase in mouse skin and human promyelocytic leukemia (HL-60) cell adhesion, inhibition of specific [3H]12-O-tetradecanoyl-phorbol-13-acetate binding to a mouse particulate fraction and activation of protein kinase C in vitro. The results showed that (+/-)-indolactam-L and (+/-)-indolactam-F had almost the same activities as (+/-)-indolactam-V, suggesting that (-)-indolactam-L and (-)-indolactam-F are new tumor promoters with as high potency as (-)-indolactam-V. (+/-)-Indolactam-t-L, which has a highly lipophilic group at C-12 of (-)-indolactam-V, showed the highest activities in the above tests. (-)-Indolactam-t-L might have stronger tumor-promoting activity than (-)-indolactam-V. Furthermore, the results with (-)-indolactam-t-L indicated the possibility of designing new tumor promoters with stronger activity than teleocidin.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Lactams,
http://linkedlifedata.com/resource/pubmed/chemical/Lyngbya Toxins,
http://linkedlifedata.com/resource/pubmed/chemical/Ornithine Decarboxylase,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase C,
http://linkedlifedata.com/resource/pubmed/chemical/Tetradecanoylphorbol Acetate,
http://linkedlifedata.com/resource/pubmed/chemical/indolactam V,
http://linkedlifedata.com/resource/pubmed/chemical/teleocidin
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0910-5050
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
78
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
577-82
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:3112073-Animals,
pubmed-meshheading:3112073-Cell Adhesion,
pubmed-meshheading:3112073-Cell Line,
pubmed-meshheading:3112073-Dose-Response Relationship, Drug,
pubmed-meshheading:3112073-Enzyme Induction,
pubmed-meshheading:3112073-Humans,
pubmed-meshheading:3112073-Indoles,
pubmed-meshheading:3112073-Lactams,
pubmed-meshheading:3112073-Leukemia, Myeloid, Acute,
pubmed-meshheading:3112073-Lyngbya Toxins,
pubmed-meshheading:3112073-Mice,
pubmed-meshheading:3112073-Neoplasms, Experimental,
pubmed-meshheading:3112073-Ornithine Decarboxylase,
pubmed-meshheading:3112073-Protein Kinase C,
pubmed-meshheading:3112073-Skin,
pubmed-meshheading:3112073-Structure-Activity Relationship,
pubmed-meshheading:3112073-Tetradecanoylphorbol Acetate
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pubmed:year |
1987
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pubmed:articleTitle |
Synthetic analogues (indolactams) of (-)-indolactam-V are new congeners of the teleocidin class of tumor promoters.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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