FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2151393992> ?p ?o ?g. }

• W2151393992 endingPage "304" @default.
• W2151393992 startingPage "297" @default.
• W2151393992 abstract "Design and synthesis ofnew derivatives of (-)-cytisine with a wide spectrum of pharmacological activity, represents the potential therapeutic interest for development of drug candidates for neurodegenerative disorders, inflammatory diseases, and treatment of nicotine addiction. We used HEK293 cell line transiently transfected with N F-κB and STATI luciferase reporter constructs to screen the (-)-cytisine derivatives for their potency to modulate basal and induced NF-κB and STAT1 activity. Currently, NF-κB, STAT1 and components of their signaling pathways are considered as attractive targets for pharmacological intervention, primarily in chronic inflammation, cancer, autoimmune, neurodegenerative and infectious diseases. The library of compounds included the derivatives of (-)-cytisine with amino-, amide-, thio- and carboxamide groups at 3, 5 and 12 position of the starting molecule, as well as some bimolecular derivatives. Our experimental data revealed compounds with moderate activating as well as inhibitory effects for basal NF-κB and STATI activity (IC50 or EC50 values are mainly in the micromolar range). The structure-activity relationship analysis demonstrated that the character of activity (activation or inhibition of NFκ-B and STAT1) is determined by the topology of the substituents at the (-)-cytisine molecule, whereas the nature of the substituents mainly contributes to severity of the effect (introduction of aromatic and adamantyl substituents, as well as thionyl or keto groups are of the principal importance). When evaluating the effect of (-)-cytisine derivatives on activity of NF-κB and STATI, induced by specific agents (TNFα and IFNγ, respectively) we observed that some compounds inhibited basal and stimulated activity of NF-κB and STAT1, another compounds showed the dual effect (an increase of basal- and a decrease of stimulated NF-κB activity) and several compounds increase both basal and induced activity of NF-κB and STAT1. Thus, obtained results suggest that one of the possible mechanisms of biological action of (-)-cytisine derivatives is their ability to influence the components of NF-κB and STAT1-dependent signaling pathways." @default.
• W2151393992 created "2016-06-24" @default.
• W2151393992 creator A5009739865 @default.
• W2151393992 creator A5015663849 @default.
• W2151393992 creator A5023026922 @default.
• W2151393992 creator A5028038450 @default.
• W2151393992 creator A5034072840 @default.
• W2151393992 creator A5064004263 @default.
• W2151393992 date "2015-05-01" @default.
• W2151393992 modified "2023-09-23" @default.
• W2151393992 title "Search for (-)-cytisine derivatives as potential inhibitors of NF-κB and STAT1" @default.
• W2151393992 cites W1881072801 @default.
• W2151393992 cites W1964227794 @default.
• W2151393992 cites W1966142717 @default.
• W2151393992 cites W1971411560 @default.
• W2151393992 cites W1972180303 @default.
• W2151393992 cites W1988487240 @default.
• W2151393992 cites W1994624766 @default.
• W2151393992 cites W2005482505 @default.
• W2151393992 cites W2020905689 @default.
• W2151393992 cites W2022143327 @default.
• W2151393992 cites W2030295894 @default.
• W2151393992 cites W2032524543 @default.
• W2151393992 cites W2038479411 @default.
• W2151393992 cites W2052372954 @default.
• W2151393992 cites W2056567434 @default.
• W2151393992 cites W2058961770 @default.
• W2151393992 cites W2059386346 @default.
• W2151393992 cites W2064163333 @default.
• W2151393992 cites W2068854551 @default.
• W2151393992 cites W2074526345 @default.
• W2151393992 cites W2080181996 @default.
• W2151393992 cites W2085278061 @default.
• W2151393992 cites W2085637535 @default.
• W2151393992 cites W2090110418 @default.
• W2151393992 cites W2104789360 @default.
• W2151393992 cites W2131046884 @default.
• W2151393992 cites W2131923232 @default.
• W2151393992 cites W2132533916 @default.
• W2151393992 cites W2138934663 @default.
• W2151393992 cites W2151650686 @default.
• W2151393992 cites W2159649016 @default.
• W2151393992 cites W2314914862 @default.
• W2151393992 cites W4237077430 @default.
• W2151393992 doi "https://doi.org/10.1134/s1068162015030103" @default.
• W2151393992 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26502610" @default.
• W2151393992 hasPublicationYear "2015" @default.
• W2151393992 type Work @default.
• W2151393992 sameAs 2151393992 @default.
• W2151393992 citedByCount "4" @default.
• W2151393992 countsByYear W21513939922016 @default.
• W2151393992 countsByYear W21513939922018 @default.
• W2151393992 countsByYear W21513939922019 @default.
• W2151393992 countsByYear W21513939922020 @default.
• W2151393992 crossrefType "journal-article" @default.
• W2151393992 hasAuthorship W2151393992A5009739865 @default.
• W2151393992 hasAuthorship W2151393992A5015663849 @default.
• W2151393992 hasAuthorship W2151393992A5023026922 @default.
• W2151393992 hasAuthorship W2151393992A5028038450 @default.
• W2151393992 hasAuthorship W2151393992A5034072840 @default.
• W2151393992 hasAuthorship W2151393992A5064004263 @default.
• W2151393992 hasConcept C116073593 @default.
• W2151393992 hasConcept C170493617 @default.
• W2151393992 hasConcept C185592680 @default.
• W2151393992 hasConcept C188987157 @default.
• W2151393992 hasConcept C202751555 @default.
• W2151393992 hasConcept C2777003663 @default.
• W2151393992 hasConcept C2777301948 @default.
• W2151393992 hasConcept C2777730290 @default.
• W2151393992 hasConcept C2778439535 @default.
• W2151393992 hasConcept C55493867 @default.
• W2151393992 hasConcept C62478195 @default.
• W2151393992 hasConcept C71924100 @default.
• W2151393992 hasConcept C98274493 @default.
• W2151393992 hasConceptScore W2151393992C116073593 @default.
• W2151393992 hasConceptScore W2151393992C170493617 @default.
• W2151393992 hasConceptScore W2151393992C185592680 @default.
• W2151393992 hasConceptScore W2151393992C188987157 @default.
• W2151393992 hasConceptScore W2151393992C202751555 @default.
• W2151393992 hasConceptScore W2151393992C2777003663 @default.
• W2151393992 hasConceptScore W2151393992C2777301948 @default.
• W2151393992 hasConceptScore W2151393992C2777730290 @default.
• W2151393992 hasConceptScore W2151393992C2778439535 @default.
• W2151393992 hasConceptScore W2151393992C55493867 @default.
• W2151393992 hasConceptScore W2151393992C62478195 @default.
• W2151393992 hasConceptScore W2151393992C71924100 @default.
• W2151393992 hasConceptScore W2151393992C98274493 @default.
• W2151393992 hasIssue "3" @default.
• W2151393992 hasLocation W21513939921 @default.
• W2151393992 hasLocation W21513939922 @default.
• W2151393992 hasOpenAccess W2151393992 @default.
• W2151393992 hasPrimaryLocation W21513939921 @default.
• W2151393992 hasRelatedWork W2024599954 @default.
• W2151393992 hasRelatedWork W2031415270 @default.
• W2151393992 hasRelatedWork W2088245318 @default.
• W2151393992 hasRelatedWork W2151393992 @default.
• W2151393992 hasRelatedWork W2315330895 @default.
• W2151393992 hasRelatedWork W2329867129 @default.

• next