FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3043171947> ?p ?o ?g. }

• W3043171947 abstract "Abstract A major cause of failure of therapy in patients with non-small cell lung cancer (NSCLC) is development of acquired drug resistance leading to tumor recurrence and disease progression. In addition to the development of new generations of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), different molecular targets may provide opportunities to improve the therapeutic outcomes. In this study, we utilized the core structure 5-fluorouracil (5-FU) or tegafur, a 5-FU prodrug combined through different linkers with resorcinol to generate a series of fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides which inhibit potent Heat Shock Protein 90 (HSP90). These compounds were found to show significant antiproliferative activity in colorectal cancer (CRC) HCT116 and NSCLC A549, H460, and H1975 (EGFR L858R/T790 M double mutation) cells. Compound 12c, developed by molecular docking analysis and enzymatic assays exhibits promising inhibitory activity of HSP90. This compound, 12c shows the most potent HSP90 inhibitory activity with an IC50 value of 27.8 ± 4.4 nM, superior to that of reference compounds AUY-922 (Luminespib) and BIIB021 whose IC50 values are 43.0 ± 0.9 nM and 56.8 ± 4.0 nM respectively. This strong HSP90 inhibitory activity of 12c leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. In addition, 12c induces significant accumulation of a sub-G1 phase population in parallel with apoptosis by showing activated caspase-3, -8 and -9 and PARP induction. These results provide a new strategy for development of novel HSP90 inhibitors for cancer treatment." @default.
• W3043171947 created "2020-07-23" @default.
• W3043171947 creator A5026553788 @default.
• W3043171947 creator A5027538061 @default.
• W3043171947 creator A5056810924 @default.
• W3043171947 creator A5057602145 @default.
• W3043171947 creator A5058719954 @default.
• W3043171947 creator A5063329944 @default.
• W3043171947 creator A5070479335 @default.
• W3043171947 creator A5072618886 @default.
• W3043171947 creator A5075105566 @default.
• W3043171947 creator A5078482756 @default.
• W3043171947 creator A5078850334 @default.
• W3043171947 date "2020-10-01" @default.
• W3043171947 modified "2023-10-17" @default.
• W3043171947 title "Fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides as antitumor agents against CRC and NSCLC cancer cells" @default.
• W3043171947 cites W1968597026 @default.
• W3043171947 cites W1980497534 @default.
• W3043171947 cites W1984328540 @default.
• W3043171947 cites W1989600727 @default.
• W3043171947 cites W1990013637 @default.
• W3043171947 cites W1994060622 @default.
• W3043171947 cites W1999715990 @default.
• W3043171947 cites W2003984225 @default.
• W3043171947 cites W2005348280 @default.
• W3043171947 cites W2010047329 @default.
• W3043171947 cites W2036236067 @default.
• W3043171947 cites W2039792930 @default.
• W3043171947 cites W2055402151 @default.
• W3043171947 cites W2072120492 @default.
• W3043171947 cites W2081801534 @default.
• W3043171947 cites W2086248882 @default.
• W3043171947 cites W2088709972 @default.
• W3043171947 cites W2091495423 @default.
• W3043171947 cites W2113523455 @default.
• W3043171947 cites W2127975859 @default.
• W3043171947 cites W2129998117 @default.
• W3043171947 cites W2130479394 @default.
• W3043171947 cites W2133735832 @default.
• W3043171947 cites W2136601558 @default.
• W3043171947 cites W2143403036 @default.
• W3043171947 cites W2158003079 @default.
• W3043171947 cites W2167512640 @default.
• W3043171947 cites W2171755671 @default.
• W3043171947 cites W2197960289 @default.
• W3043171947 cites W2317038275 @default.
• W3043171947 cites W2330241002 @default.
• W3043171947 cites W2336971858 @default.
• W3043171947 cites W2482607006 @default.
• W3043171947 cites W2509067245 @default.
• W3043171947 cites W2512471417 @default.
• W3043171947 cites W2553271730 @default.
• W3043171947 cites W2606824156 @default.
• W3043171947 cites W2739786760 @default.
• W3043171947 cites W2752676842 @default.
• W3043171947 cites W2769653645 @default.
• W3043171947 cites W2772104412 @default.
• W3043171947 cites W2792983998 @default.
• W3043171947 cites W2889502232 @default.
• W3043171947 cites W2892376819 @default.
• W3043171947 cites W2899701660 @default.
• W3043171947 cites W2906802315 @default.
• W3043171947 cites W2942625415 @default.
• W3043171947 cites W2966911669 @default.
• W3043171947 doi "https://doi.org/10.1016/j.ejmech.2020.112540" @default.
• W3043171947 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32683166" @default.
• W3043171947 hasPublicationYear "2020" @default.
• W3043171947 type Work @default.
• W3043171947 sameAs 3043171947 @default.
• W3043171947 citedByCount "5" @default.
• W3043171947 countsByYear W30431719472020 @default.
• W3043171947 countsByYear W30431719472021 @default.
• W3043171947 countsByYear W30431719472022 @default.
• W3043171947 crossrefType "journal-article" @default.
• W3043171947 hasAuthorship W3043171947A5026553788 @default.
• W3043171947 hasAuthorship W3043171947A5027538061 @default.
• W3043171947 hasAuthorship W3043171947A5056810924 @default.
• W3043171947 hasAuthorship W3043171947A5057602145 @default.
• W3043171947 hasAuthorship W3043171947A5058719954 @default.
• W3043171947 hasAuthorship W3043171947A5063329944 @default.
• W3043171947 hasAuthorship W3043171947A5070479335 @default.
• W3043171947 hasAuthorship W3043171947A5072618886 @default.
• W3043171947 hasAuthorship W3043171947A5075105566 @default.
• W3043171947 hasAuthorship W3043171947A5078482756 @default.
• W3043171947 hasAuthorship W3043171947A5078850334 @default.
• W3043171947 hasConcept C104317684 @default.
• W3043171947 hasConcept C108215921 @default.
• W3043171947 hasConcept C121608353 @default.
• W3043171947 hasConcept C126322002 @default.
• W3043171947 hasConcept C170493617 @default.
• W3043171947 hasConcept C185592680 @default.
• W3043171947 hasConcept C190283241 @default.
• W3043171947 hasConcept C202751555 @default.
• W3043171947 hasConcept C205260736 @default.
• W3043171947 hasConcept C2775932338 @default.
• W3043171947 hasConcept C2777506169 @default.
• W3043171947 hasConcept C2777560012 @default.
• W3043171947 hasConcept C2777752497 @default.
• W3043171947 hasConcept C2779438470 @default.
• W3043171947 hasConcept C502942594 @default.

• next