FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2912287316> ?p ?o ?g. }

• W2912287316 endingPage "533" @default.
• W2912287316 startingPage "515" @default.
• W2912287316 abstract "Development of hybrid drug candidates is well known strategy for designing antitumor agents. Herein, a novel class of nitric oxide donating cucurbitacin inspired estrone analogs (NO-CIEAs) were designed and synthesized as multitarget agents. Synthesized analogs were initially evaluated for their anti-hepatocellular carcinoma activities. Among the tested analogs, NO-CIEAs 17 and 20a exhibited more potent activity against HepG2 cells (IC50 = 4.69 and 12.5 µM, respectively) than the reference drug Erlotinib (IC50 = 25 µM). Interestingly, NO-CIEA 17 exerted also a high potent activity against Erlotinib-resistant HepG2 cell line (HepG2-R) (IC50 = 8.21 µM) giving insight about its importance in drug resistance therapy. Intracellular measurements of NO revealed that NO-CIEAs 17 and 20a showed a significant increase in NO production in tumor cells after 1 h of incubation comparable to the reference prodrug JS-K. Flow cytometric analysis showed that both NO-CIEAs 17 and 20a mainly arrested the HepG2 cells in the G0/G1 phase. Also, In-Cell Based ELISA screening showed that NO-CIEA 17 resulted in a potential inhibitory activity towards the EGFR and MAPK (25% and 29% inhibition compared to untreated control cells, respectively). This data suggests the binding ability of NO-CIEA 17 to the EGFR and ERK to be well correlated along with the docking and cellular studies. Also, treatment of HepG2-R cells with NO-CIEA 17 showed a potential reduction of MRP2 expression in a dose dependent manner providing a significant impact on the chemotherapeutic resistance. Overall, the current study provides a potential new approach for the discovery of a novel antitumor agent against HCC." @default.
• W2912287316 created "2019-02-21" @default.
• W2912287316 creator A5020831807 @default.
• W2912287316 creator A5069777159 @default.
• W2912287316 creator A5071522989 @default.
• W2912287316 creator A5089951361 @default.
• W2912287316 creator A5090814120 @default.
• W2912287316 date "2019-04-01" @default.
• W2912287316 modified "2023-10-16" @default.
• W2912287316 title "Design, synthesis and biological study of hybrid drug candidates of nitric oxide releasing cucurbitacin-inspired estrone analogs for treatment of hepatocellular carcinoma" @default.
• W2912287316 cites W1116726549 @default.
• W2912287316 cites W1120304398 @default.
• W2912287316 cites W1134178023 @default.
• W2912287316 cites W1965500714 @default.
• W2912287316 cites W1971561764 @default.
• W2912287316 cites W1974338599 @default.
• W2912287316 cites W1976825348 @default.
• W2912287316 cites W1982890204 @default.
• W2912287316 cites W1986107319 @default.
• W2912287316 cites W1999983083 @default.
• W2912287316 cites W2002038028 @default.
• W2912287316 cites W2004154588 @default.
• W2912287316 cites W2008059275 @default.
• W2912287316 cites W2014248078 @default.
• W2912287316 cites W2016977317 @default.
• W2912287316 cites W2017500372 @default.
• W2912287316 cites W2034666200 @default.
• W2912287316 cites W2037123220 @default.
• W2912287316 cites W2039697622 @default.
• W2912287316 cites W2040266302 @default.
• W2912287316 cites W2041763597 @default.
• W2912287316 cites W2043468314 @default.
• W2912287316 cites W2044814006 @default.
• W2912287316 cites W2055286767 @default.
• W2912287316 cites W2057589352 @default.
• W2912287316 cites W2069567767 @default.
• W2912287316 cites W2073213695 @default.
• W2912287316 cites W2076867270 @default.
• W2912287316 cites W2078625042 @default.
• W2912287316 cites W2094088741 @default.
• W2912287316 cites W2094826570 @default.
• W2912287316 cites W2104819002 @default.
• W2912287316 cites W2132395321 @default.
• W2912287316 cites W2133051701 @default.
• W2912287316 cites W2147303820 @default.
• W2912287316 cites W2159073378 @default.
• W2912287316 cites W2169244399 @default.
• W2912287316 cites W2174822994 @default.
• W2912287316 cites W2188292598 @default.
• W2912287316 cites W2251431201 @default.
• W2912287316 cites W2266511309 @default.
• W2912287316 cites W2294798900 @default.
• W2912287316 cites W2325140777 @default.
• W2912287316 cites W2333560586 @default.
• W2912287316 cites W2470538980 @default.
• W2912287316 cites W2593093801 @default.
• W2912287316 cites W2611198398 @default.
• W2912287316 cites W2618584271 @default.
• W2912287316 cites W2769260022 @default.
• W2912287316 cites W2785647304 @default.
• W2912287316 cites W2790107769 @default.
• W2912287316 cites W2790955367 @default.
• W2912287316 cites W2793026911 @default.
• W2912287316 cites W2794118112 @default.
• W2912287316 cites W2796183018 @default.
• W2912287316 cites W2800730884 @default.
• W2912287316 cites W4241110603 @default.
• W2912287316 doi "https://doi.org/10.1016/j.bioorg.2019.01.068" @default.
• W2912287316 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30807895" @default.
• W2912287316 hasPublicationYear "2019" @default.
• W2912287316 type Work @default.
• W2912287316 sameAs 2912287316 @default.
• W2912287316 citedByCount "10" @default.
• W2912287316 countsByYear W29122873162020 @default.
• W2912287316 countsByYear W29122873162021 @default.
• W2912287316 countsByYear W29122873162022 @default.
• W2912287316 countsByYear W29122873162023 @default.
• W2912287316 crossrefType "journal-article" @default.
• W2912287316 hasAuthorship W2912287316A5020831807 @default.
• W2912287316 hasAuthorship W2912287316A5069777159 @default.
• W2912287316 hasAuthorship W2912287316A5071522989 @default.
• W2912287316 hasAuthorship W2912287316A5089951361 @default.
• W2912287316 hasAuthorship W2912287316A5090814120 @default.
• W2912287316 hasConcept C108215921 @default.
• W2912287316 hasConcept C170493617 @default.
• W2912287316 hasConcept C178790620 @default.
• W2912287316 hasConcept C184235292 @default.
• W2912287316 hasConcept C185592680 @default.
• W2912287316 hasConcept C202751555 @default.
• W2912287316 hasConcept C2777752497 @default.
• W2912287316 hasConcept C2778019345 @default.
• W2912287316 hasConcept C2778087573 @default.
• W2912287316 hasConcept C2779438470 @default.
• W2912287316 hasConcept C2780035454 @default.
• W2912287316 hasConcept C502942594 @default.
• W2912287316 hasConcept C519581460 @default.
• W2912287316 hasConcept C54355233 @default.
• W2912287316 hasConcept C55493867 @default.

• next