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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
1999-8-2
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pubmed:abstractText |
Farnesyl protein transferase (FPT) is a promising target for the development of cancer chemotherapeutics because it is responsible for the farnesylation of oncogenic p21 Ras proteins which are found in nearly 30% of all human cancers and necessary for cellular development and growth. The recent discovery and progression to phase II clinical trials of trihalobenzocycloheptapyridine Sch-66336 as a potent inhibitor of FPT with oral, in vivo efficacy in mice have spawned extensive structure-activity relationship studies (SAR) of this class of compounds. Of the many trihalobenzocycloheptapyridine analogues prepared, we have identified several which inhibit FPT and cellular proliferation at single-digit nanomolar concentrations and which have good pharmacokinetic properties in mice.
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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 |
Jul
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AfonsoAA,
pubmed-author:AlvarezCC,
pubmed-author:BishopW RWR,
pubmed-author:CaroAA,
pubmed-author:ChaoJJ,
pubmed-author:DeskusJJ,
pubmed-author:DollR JRJ,
pubmed-author:GangulyA KAK,
pubmed-author:GirijavallabhanV MVM,
pubmed-author:HeimarkLL,
pubmed-author:JamesLL,
pubmed-author:KirschmeierPP,
pubmed-author:LalwaniTT,
pubmed-author:LinDD,
pubmed-author:MallamsA KAK,
pubmed-author:NjorogeF GFG,
pubmed-author:PinteFF,
pubmed-author:PramanikBB,
pubmed-author:RemiszewskiSS,
pubmed-author:RossmanR RRR,
pubmed-author:TaverasA GAG,
pubmed-author:VaccaroC JCJ,
pubmed-author:VibulbhanBB,
pubmed-author:WangLL,
pubmed-author:del RosarioJJ
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
42
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pubmed:owner |
NLM
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pubmed:authorsComplete |
N
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pubmed:pagination |
2651-61
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:10411485-Administration, Oral,
pubmed-meshheading:10411485-Alkyl and Aryl Transferases,
pubmed-meshheading:10411485-Animals,
pubmed-meshheading:10411485-Biological Availability,
pubmed-meshheading:10411485-COS Cells,
pubmed-meshheading:10411485-Cell Division,
pubmed-meshheading:10411485-Enzyme Inhibitors,
pubmed-meshheading:10411485-Haplorhini,
pubmed-meshheading:10411485-Mice,
pubmed-meshheading:10411485-Mice, Nude,
pubmed-meshheading:10411485-Piperidines,
pubmed-meshheading:10411485-Protein Prenylation,
pubmed-meshheading:10411485-Proto-Oncogene Proteins p21(ras),
pubmed-meshheading:10411485-Pyridines,
pubmed-meshheading:10411485-Structure-Activity Relationship,
pubmed-meshheading:10411485-Sulfonamides,
pubmed-meshheading:10411485-Sulfonylurea Compounds
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pubmed:year |
1999
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pubmed:articleTitle |
Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
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pubmed:affiliation |
Anti-infectives and Tumor Biology Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA.
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pubmed:publicationType |
Journal Article
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