Matches in SemOpenAlex for { <https://semopenalex.org/work/W2896867436> ?p ?o ?g. }
- W2896867436 endingPage "177" @default.
- W2896867436 startingPage "177" @default.
- W2896867436 abstract "Quinoline core has been shown to possess a promising role in the development of anticancer agents. However, the correlation between its broad spectrum of bioactivity and the underlying mechanism of actions is poorly understood. The present study, with the use of bioinformatics approaches, reported a series of designed molecules which integrated quinoline core and sulfonyl moiety, with the objective of evaluating the substituent and linker effects on anticancer activities and associated mechanistic targets. We identified potent compounds (1h, 2h, 5 and 8) exhibiting significant anticancer effects towards liver cancer cells (Hep3B) with the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) relative values of cytotoxicity below 0.40, a value in the range of doxorubicin positive control with the value of 0.12. Bulky substituents and the presence of bromine atom, as well as the presence of sulfonamide linkage, are likely the favorable structural components for molecules exerting a strong anticancer effect. To the best of our knowledge, our findings obtained from chemical synthesis, in vitro cytotoxicity, bioinformatics-based molecular docking analysis (similarity ensemble approach, SEA),and electrophoretic mobility shift assay provided the first evidence in correlation to the anticancer activities of the selected compound 5 with the modulation on the binding of transcription factor NF-κB to its target DNA. Accordingly, compound 5 represented a lead structure for the development of quinoline-based NF-κB inhibitors and this work added novel information on the understanding of the mechanism of action for bioactive sulfonyl-containing quinoline compounds against hepatocellular carcinoma." @default.
- W2896867436 created "2018-10-26" @default.
- W2896867436 creator A5003819930 @default.
- W2896867436 creator A5004337424 @default.
- W2896867436 creator A5006003842 @default.
- W2896867436 creator A5010261777 @default.
- W2896867436 creator A5020258774 @default.
- W2896867436 creator A5030568464 @default.
- W2896867436 creator A5037932562 @default.
- W2896867436 creator A5038495129 @default.
- W2896867436 creator A5041079720 @default.
- W2896867436 creator A5043847198 @default.
- W2896867436 creator A5051656994 @default.
- W2896867436 creator A5055587224 @default.
- W2896867436 creator A5056653269 @default.
- W2896867436 creator A5062082515 @default.
- W2896867436 creator A5063138704 @default.
- W2896867436 creator A5065967847 @default.
- W2896867436 creator A5066523923 @default.
- W2896867436 creator A5074425597 @default.
- W2896867436 creator A5088861689 @default.
- W2896867436 date "2018-10-22" @default.
- W2896867436 modified "2023-10-16" @default.
- W2896867436 title "Targeting DNA Binding for NF-κB as an Anticancer Approach in Hepatocellular Carcinoma" @default.
- W2896867436 cites W1663580115 @default.
- W2896867436 cites W1964693416 @default.
- W2896867436 cites W1973664779 @default.
- W2896867436 cites W1973964324 @default.
- W2896867436 cites W1975980810 @default.
- W2896867436 cites W1979262320 @default.
- W2896867436 cites W1979538859 @default.
- W2896867436 cites W1987952603 @default.
- W2896867436 cites W1989736452 @default.
- W2896867436 cites W2000640820 @default.
- W2896867436 cites W2003141219 @default.
- W2896867436 cites W2004695394 @default.
- W2896867436 cites W2017194759 @default.
- W2896867436 cites W2023622490 @default.
- W2896867436 cites W2031521984 @default.
- W2896867436 cites W2034661714 @default.
- W2896867436 cites W2036129809 @default.
- W2896867436 cites W2039926931 @default.
- W2896867436 cites W2040935952 @default.
- W2896867436 cites W2048008261 @default.
- W2896867436 cites W2062070836 @default.
- W2896867436 cites W2063670001 @default.
- W2896867436 cites W2065713235 @default.
- W2896867436 cites W2071551353 @default.
- W2896867436 cites W2075482188 @default.
- W2896867436 cites W2077449511 @default.
- W2896867436 cites W2079981504 @default.
- W2896867436 cites W2096271097 @default.
- W2896867436 cites W2098107650 @default.
- W2896867436 cites W2103142972 @default.
- W2896867436 cites W2105668062 @default.
- W2896867436 cites W2108197429 @default.
- W2896867436 cites W2118986158 @default.
- W2896867436 cites W2132629607 @default.
- W2896867436 cites W2136095930 @default.
- W2896867436 cites W2142384246 @default.
- W2896867436 cites W2158734599 @default.
- W2896867436 cites W2162011385 @default.
- W2896867436 cites W2169678694 @default.
- W2896867436 cites W2179203678 @default.
- W2896867436 cites W2180209922 @default.
- W2896867436 cites W2287340535 @default.
- W2896867436 cites W2290077561 @default.
- W2896867436 cites W2325270524 @default.
- W2896867436 cites W2327053736 @default.
- W2896867436 cites W2410126920 @default.
- W2896867436 cites W2477430054 @default.
- W2896867436 cites W2605478093 @default.
- W2896867436 cites W2757414588 @default.
- W2896867436 cites W2767718521 @default.
- W2896867436 cites W2771428152 @default.
- W2896867436 cites W2794661317 @default.
- W2896867436 cites W2805459097 @default.
- W2896867436 cites W2891699854 @default.
- W2896867436 cites W2950940645 @default.
- W2896867436 cites W401839946 @default.
- W2896867436 cites W588559152 @default.
- W2896867436 doi "https://doi.org/10.3390/cells7100177" @default.
- W2896867436 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6209864" @default.
- W2896867436 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30360426" @default.
- W2896867436 hasPublicationYear "2018" @default.
- W2896867436 type Work @default.
- W2896867436 sameAs 2896867436 @default.
- W2896867436 citedByCount "11" @default.
- W2896867436 countsByYear W28968674362019 @default.
- W2896867436 countsByYear W28968674362020 @default.
- W2896867436 countsByYear W28968674362021 @default.
- W2896867436 countsByYear W28968674362022 @default.
- W2896867436 countsByYear W28968674362023 @default.
- W2896867436 crossrefType "journal-article" @default.
- W2896867436 hasAuthorship W2896867436A5003819930 @default.
- W2896867436 hasAuthorship W2896867436A5004337424 @default.
- W2896867436 hasAuthorship W2896867436A5006003842 @default.
- W2896867436 hasAuthorship W2896867436A5010261777 @default.