FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2475360018> ?p ?o ?g. }

• W2475360018 endingPage "129" @default.
• W2475360018 startingPage "116" @default.
• W2475360018 abstract "A new series of 3-substituted-4-hydroxycoumarin derivatives was designed, synthesized, and evaluated for CDK inhibiting and anticancer activities. All the synthesized target compounds showed remarkably high affinity and selectivity towards CDK1B, compared to flavopiridol, with Ki values in the low nanomolar range (Ki=0.35-0.88nM). Most of them elicited considerable inhibiting effect against CDK9T1 (Ki=3.26-23.45nM). Moreover, all the target compounds were tested in vitro against eighteen types of human tumor cell lines. The hydrazone 3a, N-phenylpyrazoline derivative 6b and 2-aminopyridyl-3-carbonitrile derivative 8c were the most potent anticancer agents against MCF-7 breast cancer cell line (IC50=0.21, 0.21 and 0.23nM, respectively). The target compounds 3a, 6b and 8c were further evaluated in MCF-7 breast cancer mouse xenograft model and showed in vivo efficacy at 10mg/kg dose. The docking study confirmed a unique binding mode in the active site of CDK1B with better score than flavopiridol. Quantitative structure activity relationship study was done and revealed a highly predictive power R(2) of 0.81." @default.
• W2475360018 created "2016-07-22" @default.
• W2475360018 creator A5004476989 @default.
• W2475360018 creator A5065622587 @default.
• W2475360018 creator A5085190660 @default.
• W2475360018 creator A5089347460 @default.
• W2475360018 date "2016-08-01" @default.
• W2475360018 modified "2023-10-13" @default.
• W2475360018 title "3-Substituted-4-hydroxycoumarin as a new scaffold with potent CDK inhibition and promising anticancer effect: Synthesis, molecular modeling and QSAR studies" @default.
• W2475360018 cites W1970430170 @default.
• W2475360018 cites W1973932125 @default.
• W2475360018 cites W1982308040 @default.
• W2475360018 cites W1984048729 @default.
• W2475360018 cites W1985389450 @default.
• W2475360018 cites W1986262384 @default.
• W2475360018 cites W1991054314 @default.
• W2475360018 cites W1992446399 @default.
• W2475360018 cites W2002235730 @default.
• W2475360018 cites W2007887352 @default.
• W2475360018 cites W2017120709 @default.
• W2475360018 cites W2018667895 @default.
• W2475360018 cites W2020667637 @default.
• W2475360018 cites W2023587394 @default.
• W2475360018 cites W2024745849 @default.
• W2475360018 cites W2025813673 @default.
• W2475360018 cites W2028579197 @default.
• W2475360018 cites W2028640652 @default.
• W2475360018 cites W2028793394 @default.
• W2475360018 cites W2029080338 @default.
• W2475360018 cites W2035027593 @default.
• W2475360018 cites W2035273416 @default.
• W2475360018 cites W2039771541 @default.
• W2475360018 cites W2042541486 @default.
• W2475360018 cites W2043750458 @default.
• W2475360018 cites W2046024621 @default.
• W2475360018 cites W2063193324 @default.
• W2475360018 cites W2063644591 @default.
• W2475360018 cites W2066107979 @default.
• W2475360018 cites W2066360911 @default.
• W2475360018 cites W2074631079 @default.
• W2475360018 cites W2074918415 @default.
• W2475360018 cites W2077196962 @default.
• W2475360018 cites W2082095457 @default.
• W2475360018 cites W2084370215 @default.
• W2475360018 cites W2085593164 @default.
• W2475360018 cites W2088202453 @default.
• W2475360018 cites W2090564505 @default.
• W2475360018 cites W2113662093 @default.
• W2475360018 cites W2114918609 @default.
• W2475360018 cites W2127549020 @default.
• W2475360018 cites W2129679336 @default.
• W2475360018 cites W2139899373 @default.
• W2475360018 cites W2140642045 @default.
• W2475360018 cites W2144002245 @default.
• W2475360018 cites W2172390093 @default.
• W2475360018 cites W2951407519 @default.
• W2475360018 doi "https://doi.org/10.1016/j.bioorg.2016.06.005" @default.
• W2475360018 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27372186" @default.
• W2475360018 hasPublicationYear "2016" @default.
• W2475360018 type Work @default.
• W2475360018 sameAs 2475360018 @default.
• W2475360018 citedByCount "42" @default.
• W2475360018 countsByYear W24753600182017 @default.
• W2475360018 countsByYear W24753600182018 @default.
• W2475360018 countsByYear W24753600182019 @default.
• W2475360018 countsByYear W24753600182020 @default.
• W2475360018 countsByYear W24753600182021 @default.
• W2475360018 countsByYear W24753600182022 @default.
• W2475360018 countsByYear W24753600182023 @default.
• W2475360018 crossrefType "journal-article" @default.
• W2475360018 hasAuthorship W2475360018A5004476989 @default.
• W2475360018 hasAuthorship W2475360018A5065622587 @default.
• W2475360018 hasAuthorship W2475360018A5085190660 @default.
• W2475360018 hasAuthorship W2475360018A5089347460 @default.
• W2475360018 hasConcept C150903083 @default.
• W2475360018 hasConcept C159110408 @default.
• W2475360018 hasConcept C164126121 @default.
• W2475360018 hasConcept C185592680 @default.
• W2475360018 hasConcept C193042331 @default.
• W2475360018 hasConcept C202751555 @default.
• W2475360018 hasConcept C207001950 @default.
• W2475360018 hasConcept C21951064 @default.
• W2475360018 hasConcept C2777752112 @default.
• W2475360018 hasConcept C2777752497 @default.
• W2475360018 hasConcept C2780349576 @default.
• W2475360018 hasConcept C41685203 @default.
• W2475360018 hasConcept C54355233 @default.
• W2475360018 hasConcept C55493867 @default.
• W2475360018 hasConcept C71240020 @default.
• W2475360018 hasConcept C71924100 @default.
• W2475360018 hasConcept C81885089 @default.
• W2475360018 hasConcept C86803240 @default.
• W2475360018 hasConcept C98274493 @default.
• W2475360018 hasConceptScore W2475360018C150903083 @default.
• W2475360018 hasConceptScore W2475360018C159110408 @default.
• W2475360018 hasConceptScore W2475360018C164126121 @default.
• W2475360018 hasConceptScore W2475360018C185592680 @default.
• W2475360018 hasConceptScore W2475360018C193042331 @default.

• next