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rdf:type |
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lifeskim:mentions |
umls-concept:C0002482,
umls-concept:C0034251,
umls-concept:C0057888,
umls-concept:C0138837,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0243072,
umls-concept:C0243077,
umls-concept:C0332256,
umls-concept:C0441655,
umls-concept:C1260969,
umls-concept:C1883254
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pubmed:issue |
18
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pubmed:dateCreated |
1999-2-2
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pubmed:abstractText |
Bioisosteric replacement of the C-6 carbon atom in piperidine I and piperazine II with S, O, and N heteroatoms is described. Amide and cyanoguanidine derivatives of these compounds were evaluated in vitro and found to be good inhibitors of farnesyl-protein transferase. An improved method of preparing the 5,11-dihydro-[1]-benzthiepin nucleus 6 was accomplished in high yield and with excellent regioselectivity using an AlCl3 melt protocol.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Alkyl and Aryl Transferases,
http://linkedlifedata.com/resource/pubmed/chemical/Amides,
http://linkedlifedata.com/resource/pubmed/chemical/Benzazepines,
http://linkedlifedata.com/resource/pubmed/chemical/Benzoxepins,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Guanidines,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/dicyandiamido,
http://linkedlifedata.com/resource/pubmed/chemical/p21(ras) farnesyl-protein...
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2521-6
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:9873573-Alkyl and Aryl Transferases,
pubmed-meshheading:9873573-Amides,
pubmed-meshheading:9873573-Benzazepines,
pubmed-meshheading:9873573-Benzoxepins,
pubmed-meshheading:9873573-Enzyme Inhibitors,
pubmed-meshheading:9873573-Guanidines,
pubmed-meshheading:9873573-Models, Chemical,
pubmed-meshheading:9873573-Piperazines,
pubmed-meshheading:9873573-Piperidines,
pubmed-meshheading:9873573-Protein Prenylation,
pubmed-meshheading:9873573-Pyridines,
pubmed-meshheading:9873573-Structure-Activity Relationship
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pubmed:year |
1998
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pubmed:articleTitle |
Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.
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pubmed:affiliation |
Schering-Plough Research Institute, Department of Chemistry, Kenilworth, New Jersey 07033, USA.
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pubmed:publicationType |
Journal Article
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