| pubmed-article:17154501 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:17154501 | lifeskim:mentions | umls-concept:C0035647 | lld:lifeskim |
| pubmed-article:17154501 | lifeskim:mentions | umls-concept:C0162638 | lld:lifeskim |
| pubmed-article:17154501 | lifeskim:mentions | umls-concept:C0010656 | lld:lifeskim |
| pubmed-article:17154501 | lifeskim:mentions | umls-concept:C0022115 | lld:lifeskim |
| pubmed-article:17154501 | lifeskim:mentions | umls-concept:C1537028 | lld:lifeskim |
| pubmed-article:17154501 | lifeskim:mentions | umls-concept:C0336791 | lld:lifeskim |
| pubmed-article:17154501 | pubmed:issue | 23 | lld:pubmed |
| pubmed-article:17154501 | pubmed:dateCreated | 2006-12-12 | lld:pubmed |
| pubmed-article:17154501 | pubmed:abstractText | Caspases are the unique enzymes responsible for the execution of the cell death program and may represent an exclusive target for the specific molecular imaging of apoptosis in vivo. 5-Pyrrolidinylsulfonyl isatins represent potent nonpeptidyl caspase inhibitors that may be suitable for the development of caspase binding radioligands (CBRs). (S)-5-[1-(2-Methoxymethylpyrrolidinyl)sulfonyl]isatin (7) served as a lead compound for modification of its N-1-position. Corresponding pairs of N-1-substituted 2-methoxymethyl- and 2-phenoxymethylpyrrolidinyl derivatives were examined in vitro by biochemical caspase inhibition assays. All target compounds possess high in vitro caspase inhibition potencies in the nanomolar to subnanomolar range for caspase-3 (Ki=0.2-56.1 nM). As shown for compound (S)-1-(4-(2-fluoroethoxy)benzyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin (35), the class of N-1-substituted 5-pyrrolidinylsulfonyl isatins competitively inhibits caspase-3. All caspase inhibitors show selectivity for the effector caspases-3 and -7 in vitro. The 2-methoxymethylpyrrolidinyl versions of the isatins appear to possess superior caspase inhibition potencies in cellular apoptosis inhibition assays compared with the 2-phenoxymethylpyrrolidinyl inhibitors. | lld:pubmed |
| pubmed-article:17154501 | pubmed:language | eng | lld:pubmed |
| pubmed-article:17154501 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17154501 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:17154501 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17154501 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17154501 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17154501 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:17154501 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17154501 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:17154501 | pubmed:month | Nov | lld:pubmed |
| pubmed-article:17154501 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:LevkauBodoB | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:SchoberOtmarO | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:SchäfersMicha... | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:WagnerStefanS | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:KopkaKlausK | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:BreyholzHans-... | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:KeulPetraP | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:HöltkeCarsten... | lld:pubmed |
| pubmed-article:17154501 | pubmed:author | pubmed-author:FaustAndreasA | lld:pubmed |
| pubmed-article:17154501 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:17154501 | pubmed:day | 16 | lld:pubmed |
| pubmed-article:17154501 | pubmed:volume | 49 | lld:pubmed |
| pubmed-article:17154501 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:17154501 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:17154501 | pubmed:pagination | 6704-15 | lld:pubmed |
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| pubmed-article:17154501 | pubmed:meshHeading | pubmed-meshheading:17154501... | lld:pubmed |
| pubmed-article:17154501 | pubmed:year | 2006 | lld:pubmed |
| pubmed-article:17154501 | pubmed:articleTitle | 5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis. | lld:pubmed |
| pubmed-article:17154501 | pubmed:affiliation | Department of Nuclear Medicine, University Hospital of the Westfälische Wilhelms-Universität, Münster, Germany. kopka@uni-muenster.de | lld:pubmed |
| pubmed-article:17154501 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:17154501 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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