| pubmed-article:17881236 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:17881236 | lifeskim:mentions | umls-concept:C0733755 | lld:lifeskim |
| pubmed-article:17881236 | lifeskim:mentions | umls-concept:C1130454 | lld:lifeskim |
| pubmed-article:17881236 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:17881236 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:17881236 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:17881236 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:17881236 | lifeskim:mentions | umls-concept:C0597413 | lld:lifeskim |
| pubmed-article:17881236 | pubmed:issue | 24 | lld:pubmed |
| pubmed-article:17881236 | pubmed:dateCreated | 2007-10-22 | lld:pubmed |
| pubmed-article:17881236 | pubmed:abstractText | Nucleoside transporter inhibitors have potential therapeutic applications as anticancer, antiviral, cardioprotective, and neuroprotective agents. S(6)-(4-nitrobenzyl)mercaptopurine riboside (NBMPR) is a prototype inhibitor of the human equilibrative nucleoside transporter (hENT1), and is a high affinity ligand with a K(d) of 0.1-1.0 nM. We have synthesized and flow cytometrically evaluated the binding affinity of a series of novel C(2)-purine position substituted analogs of NBMPR at the hENT1. The aim of this research was to understand the substituent requirements at the C(2)-purine position of NBMPR. Structure-activity relationships (SAR) indicate that increasing the steric bulk at the C(2)-purine position of NBMPR led to a decrease in binding affinity of these ligands at the hENT1. New high affinity inhibitors were identified, with the best compound, 2-fluoro-4-nitrobenzyl mercaptopurine riboside (7), exhibiting a K(i) of 2.1 nM. This information, when coupled with the information obtained from other structure-activity relationship studies should prove useful in efforts aimed at modeling the NMBPR and analogs pharmacophore of hENT1 inhibitors. | lld:pubmed |
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| pubmed-article:17881236 | pubmed:language | eng | lld:pubmed |
| pubmed-article:17881236 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17881236 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:17881236 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:17881236 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:17881236 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:17881236 | pubmed:issn | 1464-3391 | lld:pubmed |
| pubmed-article:17881236 | pubmed:author | pubmed-author:BuolamwiniJoh... | lld:pubmed |
| pubmed-article:17881236 | pubmed:author | pubmed-author:GupteAmolA | lld:pubmed |
| pubmed-article:17881236 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:17881236 | pubmed:day | 15 | lld:pubmed |
| pubmed-article:17881236 | pubmed:volume | 15 | lld:pubmed |
| pubmed-article:17881236 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:17881236 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:17881236 | pubmed:pagination | 7726-37 | lld:pubmed |
| pubmed-article:17881236 | pubmed:dateRevised | 2011-9-26 | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:meshHeading | pubmed-meshheading:17881236... | lld:pubmed |
| pubmed-article:17881236 | pubmed:year | 2007 | lld:pubmed |
| pubmed-article:17881236 | pubmed:articleTitle | Novel C2-purine position analogs of nitrobenzylmercaptopurine riboside as human equilibrative nucleoside transporter 1 inhibitors. | lld:pubmed |
| pubmed-article:17881236 | pubmed:affiliation | Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Sciences Center, 847 Monroe Avenue Suite 327, Memphis, TN 38163, USA. | lld:pubmed |
| pubmed-article:17881236 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:17881236 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:17881236 | lld:chembl |
