FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2003417794> ?p ?o ?g. }

• W2003417794 endingPage "3789" @default.
• W2003417794 startingPage "3774" @default.
• W2003417794 abstract "Potent nonpeptidic benzimidazole sulfonamide inhibitors of protein tyrosine phosphatase 1B (PTP1B) were derived from the optimization of a tripeptide containing the novel (S)-isothiazolidinone ((S)-IZD) phosphotyrosine (pTyr) mimetic. An X-ray cocrystal structure of inhibitor 46/PTP1B at 1.8 A resolution demonstrated that the benzimidazole sulfonamides form a bidentate H bond to Asp48 as designed, although the aryl group of the sulfonamide unexpectedly interacts intramolecularly in a pi-stacking manner with the benzimidazole. The ortho substitution to the (S)-IZD on the aryl ring afforded low nanomolar enzyme inhibitors of PTP1B that also displayed low caco-2 permeability and cellular activity in an insulin receptor (IR) phosphorylation assay and an Akt phosphorylation assay. The design, synthesis, and SAR of this novel series of benzimidazole sulfonamide containing (S)-IZD inhibitors of PTP1B are presented herein." @default.
• W2003417794 created "2016-06-24" @default.
• W2003417794 creator A5007836468 @default.
• W2003417794 creator A5011396195 @default.
• W2003417794 creator A5014416581 @default.
• W2003417794 creator A5017603782 @default.
• W2003417794 creator A5022438790 @default.
• W2003417794 creator A5022865195 @default.
• W2003417794 creator A5023418454 @default.
• W2003417794 creator A5027467988 @default.
• W2003417794 creator A5034132730 @default.
• W2003417794 creator A5036359487 @default.
• W2003417794 creator A5041230347 @default.
• W2003417794 creator A5041340848 @default.
• W2003417794 creator A5041451706 @default.
• W2003417794 creator A5045592607 @default.
• W2003417794 creator A5045701763 @default.
• W2003417794 creator A5058147530 @default.
• W2003417794 creator A5058291576 @default.
• W2003417794 creator A5059677466 @default.
• W2003417794 creator A5064375039 @default.
• W2003417794 creator A5066209236 @default.
• W2003417794 creator A5067823470 @default.
• W2003417794 creator A5074781214 @default.
• W2003417794 creator A5076639320 @default.
• W2003417794 creator A5077129573 @default.
• W2003417794 creator A5079340548 @default.
• W2003417794 creator A5083124630 @default.
• W2003417794 creator A5090696087 @default.
• W2003417794 date "2006-06-01" @default.
• W2003417794 modified "2023-09-26" @default.
• W2003417794 title "Potent Benzimidazole Sulfonamide Protein Tyrosine Phosphatase 1B Inhibitors Containing the Heterocyclic (<i>S</i>)-Isothiazolidinone Phosphotyrosine Mimetic" @default.
• W2003417794 cites W2005239250 @default.
• W2003417794 cites W2030156849 @default.
• W2003417794 cites W2039390437 @default.
• W2003417794 cites W2054652820 @default.
• W2003417794 cites W2070980519 @default.
• W2003417794 cites W2094069133 @default.
• W2003417794 cites W2115681043 @default.
• W2003417794 cites W2123229219 @default.
• W2003417794 cites W2133637497 @default.
• W2003417794 cites W2157971107 @default.
• W2003417794 doi "https://doi.org/10.1021/jm0600904" @default.
• W2003417794 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16789735" @default.
• W2003417794 hasPublicationYear "2006" @default.
• W2003417794 type Work @default.
• W2003417794 sameAs 2003417794 @default.
• W2003417794 citedByCount "81" @default.
• W2003417794 countsByYear W20034177942012 @default.
• W2003417794 countsByYear W20034177942013 @default.
• W2003417794 countsByYear W20034177942014 @default.
• W2003417794 countsByYear W20034177942015 @default.
• W2003417794 countsByYear W20034177942016 @default.
• W2003417794 countsByYear W20034177942017 @default.
• W2003417794 countsByYear W20034177942018 @default.
• W2003417794 countsByYear W20034177942019 @default.
• W2003417794 countsByYear W20034177942020 @default.
• W2003417794 countsByYear W20034177942021 @default.
• W2003417794 countsByYear W20034177942022 @default.
• W2003417794 crossrefType "journal-article" @default.
• W2003417794 hasAuthorship W2003417794A5007836468 @default.
• W2003417794 hasAuthorship W2003417794A5011396195 @default.
• W2003417794 hasAuthorship W2003417794A5014416581 @default.
• W2003417794 hasAuthorship W2003417794A5017603782 @default.
• W2003417794 hasAuthorship W2003417794A5022438790 @default.
• W2003417794 hasAuthorship W2003417794A5022865195 @default.
• W2003417794 hasAuthorship W2003417794A5023418454 @default.
• W2003417794 hasAuthorship W2003417794A5027467988 @default.
• W2003417794 hasAuthorship W2003417794A5034132730 @default.
• W2003417794 hasAuthorship W2003417794A5036359487 @default.
• W2003417794 hasAuthorship W2003417794A5041230347 @default.
• W2003417794 hasAuthorship W2003417794A5041340848 @default.
• W2003417794 hasAuthorship W2003417794A5041451706 @default.
• W2003417794 hasAuthorship W2003417794A5045592607 @default.
• W2003417794 hasAuthorship W2003417794A5045701763 @default.
• W2003417794 hasAuthorship W2003417794A5058147530 @default.
• W2003417794 hasAuthorship W2003417794A5058291576 @default.
• W2003417794 hasAuthorship W2003417794A5059677466 @default.
• W2003417794 hasAuthorship W2003417794A5064375039 @default.
• W2003417794 hasAuthorship W2003417794A5066209236 @default.
• W2003417794 hasAuthorship W2003417794A5067823470 @default.
• W2003417794 hasAuthorship W2003417794A5074781214 @default.
• W2003417794 hasAuthorship W2003417794A5076639320 @default.
• W2003417794 hasAuthorship W2003417794A5077129573 @default.
• W2003417794 hasAuthorship W2003417794A5079340548 @default.
• W2003417794 hasAuthorship W2003417794A5083124630 @default.
• W2003417794 hasAuthorship W2003417794A5090696087 @default.
• W2003417794 hasConcept C11960822 @default.
• W2003417794 hasConcept C178790620 @default.
• W2003417794 hasConcept C185592680 @default.
• W2003417794 hasConcept C2778484023 @default.
• W2003417794 hasConcept C2780263894 @default.
• W2003417794 hasConcept C2781039511 @default.
• W2003417794 hasConcept C2781076698 @default.
• W2003417794 hasConcept C55493867 @default.
• W2003417794 hasConcept C71240020 @default.
• W2003417794 hasConcept C85528070 @default.
• W2003417794 hasConceptScore W2003417794C11960822 @default.

• next