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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2009-5-18
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pubmed:abstractText |
Chiral and achiral macrocyclic bis-diketal diamines, analogs of bicyclam AMD 3100, were synthesized in three steps from the previously obtained 14-membered ring diketal dilactams. Their monoreduction with lithium aluminium hydride gave the corresponding diketal aminolactams. Coupling these with dibromo-p-xylene led to xylyl dimer compounds. A second reduction step yielded the expected bis-diketal diamines in the methyl and unsubstituted series. Biological tests on the unreduced and reduced dimers showed both weak anti-HIV and anti-proliferative activities for the bis-diphenyl diketal aminolactam 13b, with a mode of action probably different from that of AMD 3100.
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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 |
|
|
pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1768-3254
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pubmed:author |
|
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pubmed:issnType |
Electronic
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pubmed:volume |
44
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3138-46
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pubmed:meshHeading |
pubmed-meshheading:19356827-Animals,
pubmed-meshheading:19356827-Anti-HIV Agents,
pubmed-meshheading:19356827-Antineoplastic Agents,
pubmed-meshheading:19356827-Cell Line, Tumor,
pubmed-meshheading:19356827-Cell Proliferation,
pubmed-meshheading:19356827-Diamines,
pubmed-meshheading:19356827-Heterocyclic Compounds,
pubmed-meshheading:19356827-Humans,
pubmed-meshheading:19356827-Inhibitory Concentration 50,
pubmed-meshheading:19356827-Lactams, Macrocyclic,
pubmed-meshheading:19356827-Molecular Conformation,
pubmed-meshheading:19356827-Oxygen
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pubmed:year |
2009
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|
pubmed:articleTitle |
Bis-14-membered ring diketal diamines: synthesis and evaluation of their anti-HIV and anti-tumoral activities.
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pubmed:affiliation |
Laboratoire Synthèse Et Etude de Systèmes à Intérêt Biologique, UMR CNRS 6504, Université Blaise Pascal de Clermont-Ferrand, Aubière, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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