| pubmed-article:19140683 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:19140683 | lifeskim:mentions | umls-concept:C0282519 | lld:lifeskim |
| pubmed-article:19140683 | lifeskim:mentions | umls-concept:C0441655 | lld:lifeskim |
| pubmed-article:19140683 | lifeskim:mentions | umls-concept:C0596988 | lld:lifeskim |
| pubmed-article:19140683 | lifeskim:mentions | umls-concept:C1880355 | lld:lifeskim |
| pubmed-article:19140683 | lifeskim:mentions | umls-concept:C2347946 | lld:lifeskim |
| pubmed-article:19140683 | lifeskim:mentions | umls-concept:C0121925 | lld:lifeskim |
| pubmed-article:19140683 | lifeskim:mentions | umls-concept:C0243072 | lld:lifeskim |
| pubmed-article:19140683 | pubmed:issue | 3 | lld:pubmed |
| pubmed-article:19140683 | pubmed:dateCreated | 2009-2-5 | lld:pubmed |
| pubmed-article:19140683 | pubmed:abstractText | The role played by stereochemistry in the C2-substituent (left part) on the S-DABO scaffold for anti-HIV-1 activity has been investigated for the first time. A series of S-DABO analogues, where the double bond in the C2-substituent is replaced by an enantiopure isosteric cyclopropyl moiety, has been synthesized, leading to the identification of a potent lead compound endowed with picomolar activity against RT (wt) and nanomolar activity against selected drug-resistant mutants. Molecular modeling calculation, enzymatic studies, and surface plasmon resonance experiments allowed us to rationalize the biological behavior of the synthesized compounds, which act as mixed-type inhibitors of HIV-1 RT K103N, with a preferential association to the enzyme-substrate complex. Taken together, our data show that the right combination of stereochemistry on the left and right parts (C6-substituent) of the S-DABO scaffold plays a key role in the inhibition of both wild-type and drug-resistant enzymes, especially the K103N mutant. | lld:pubmed |
| pubmed-article:19140683 | pubmed:language | eng | lld:pubmed |
| pubmed-article:19140683 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19140683 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:19140683 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19140683 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19140683 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19140683 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19140683 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19140683 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:19140683 | pubmed:month | Feb | lld:pubmed |
| pubmed-article:19140683 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:EstéJosé AJA | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:BottaMaurizio... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:GiorgiGianluc... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:TafiAndreaA | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:MagaGiovanniG | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:EnnifarEricE | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:DumasPhilippe... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:Armand-UgonMe... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:BecGuillaumeG | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:GonzalezEmman... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:SamueleAlbert... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:RadiMarcoM | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:BaltzingerMir... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:ZanoliSamanth... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:BellucciLucaL | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:AlongiMaddale... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:AngeliLucilla... | lld:pubmed |
| pubmed-article:19140683 | pubmed:author | pubmed-author:CasaluceGiann... | lld:pubmed |
| pubmed-article:19140683 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:19140683 | pubmed:day | 12 | lld:pubmed |
| pubmed-article:19140683 | pubmed:volume | 52 | lld:pubmed |
| pubmed-article:19140683 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:19140683 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:19140683 | pubmed:pagination | 840-51 | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:meshHeading | pubmed-meshheading:19140683... | lld:pubmed |
| pubmed-article:19140683 | pubmed:year | 2009 | lld:pubmed |
| pubmed-article:19140683 | pubmed:articleTitle | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. | lld:pubmed |
| pubmed-article:19140683 | pubmed:affiliation | Dipartimento Farmaco Chimico Tecnologico, University of Siena,Via Alcide de Gasperi 2, I-53100 Siena, Italy. | lld:pubmed |
| pubmed-article:19140683 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:19140683 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:19140683 | lld:chembl |
