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rdf:type |
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|
lifeskim:mentions |
|
|
pubmed:issue |
10
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pubmed:dateCreated |
1996-7-18
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|
pubmed:abstractText |
A series of novel aminodiol inhibitors of HIV protease based on the lead compound 1 with structural modifications at P1' were synthesized in order to reduce the cytotoxicity of 1. We have observed a high degree of correlation between the lipophilicity and cytotoxicity of this series of inhibitors. It was found that appropriate substitution at the para position of the P1' phenyl group of 1 resulted in the identification of equipotent (both against the enzyme and in cell culture) compounds (10l, 10m, 10n, and 15c) which possess significantly decreased cytotoxicity.
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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 |
May
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AlamMM,
pubmed-author:BarrishJ CJC,
pubmed-author:BeyerB DBD,
pubmed-author:BisacchiG SGS,
pubmed-author:ChenPP,
pubmed-author:ChengP TPT,
pubmed-author:ColonnoR JRJ,
pubmed-author:DejnekaTT,
pubmed-author:EvansA JAJ,
pubmed-author:GreytokJ AJA,
pubmed-author:HermsmeierM AMA,
pubmed-author:HumphreysW GWG,
pubmed-author:JacobsG AGA,
pubmed-author:KocyOO,
pubmed-author:LimP GPG,
pubmed-author:LisK AKA,
pubmed-author:MarellaM AMA,
pubmed-author:RoyA CAC,
pubmed-author:RyonoD EDE,
pubmed-author:SheafferA KAK,
pubmed-author:SpergelS HSH,
pubmed-author:TinoJ AJA,
pubmed-author:ViteGG,
pubmed-author:ZahlerRR
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|
pubmed:issnType |
Print
|
|
pubmed:day |
10
|
|
pubmed:volume |
39
|
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pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
1991-2007
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|
pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
|
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pubmed:year |
1996
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pubmed:articleTitle |
Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.
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pubmed:affiliation |
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-4000, USA.
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pubmed:publicationType |
Journal Article
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