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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
1998-8-17
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pubmed:abstractText |
Four new hybrid analogues of 1alpha,25-dihydroxyvitamin D3 (1) have been synthesized in a convergent manner by joining A-ring and C, D-ring fragments. Each hybrid analogue, having a noncalcemic 1-hydroxymethyl group and a potentiating 16-ene 24,24-difluorinated C,D-ring side chain, was designed to be lipophilic and inert toward 24-hydroxylase enzyme catabolism. Each hybrid analogue with 1beta, 3alpha-substituent stereochemistry (i.e., analogues 3b and 4b) showed a pharmacologically desirable combination of in vitro high antiproliferative activity in two different cell lines and high transcriptional activity with also low calcemic activity in vivo.
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pubmed:grant |
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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 |
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pubmed:issnType |
Print
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pubmed:day |
30
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pubmed:volume |
41
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3008-14
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pubmed:dateRevised |
2008-8-16
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pubmed:meshHeading |
pubmed-meshheading:9685240-Administration, Oral,
pubmed-meshheading:9685240-Animals,
pubmed-meshheading:9685240-Antineoplastic Agents,
pubmed-meshheading:9685240-Calcitriol,
pubmed-meshheading:9685240-Calcium,
pubmed-meshheading:9685240-Cell Division,
pubmed-meshheading:9685240-Circular Dichroism,
pubmed-meshheading:9685240-Cytochrome P-450 Enzyme System,
pubmed-meshheading:9685240-Drug Screening Assays, Antitumor,
pubmed-meshheading:9685240-Keratinocytes,
pubmed-meshheading:9685240-Magnetic Resonance Spectroscopy,
pubmed-meshheading:9685240-Male,
pubmed-meshheading:9685240-Mice,
pubmed-meshheading:9685240-Rats,
pubmed-meshheading:9685240-Rats, Inbred F344,
pubmed-meshheading:9685240-Stereoisomerism,
pubmed-meshheading:9685240-Steroid Hydroxylases,
pubmed-meshheading:9685240-Transcription, Genetic,
pubmed-meshheading:9685240-Transfection,
pubmed-meshheading:9685240-Tumor Cells, Cultured
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pubmed:year |
1998
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pubmed:articleTitle |
Noncalcemic, antiproliferative, transcriptionally active, 24-fluorinated hybrid analogues of the hormone 1alpha, 25-dihydroxyvitamin D3. Synthesis and preliminary biological evaluation.
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pubmed:affiliation |
Department of Chemistry, Johns Hopkins University, Baltimore, Maryland 21218, Department of Medical Specialities, The University of Texas, M. D. Anderson Cancer Center, Houston, Texas 77030, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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