FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4318473113> ?p ?o ?g. }

• W4318473113 endingPage "1308" @default.
• W4318473113 startingPage "1308" @default.
• W4318473113 abstract "A series of novel 3,9-disubstituted acridines were synthesized and their biological potential was investigated. The synthetic plan consists of eight reaction steps, which produce the final products, derivatives 17a–17j, in a moderate yield. The principles of cheminformatics and computational chemistry were applied in order to study the relationship between the physicochemical properties of the 3,9-disubstituted acridines and their biological activity at a cellular and molecular level. The selected 3,9-disubstituted acridine derivatives were studied in the presence of DNA using spectroscopic (UV-Vis, circular dichroism, and thermal denaturation) and electrophoretic (nuclease activity, relaxation and unwinding assays for topoisomerase I and decatenation assay for topoisomerase IIα) methods. Binding constants (2.81–9.03 × 104 M−1) were calculated for the derivatives from the results of the absorption titration spectra. The derivatives were found to have caused the inhibition of both topoisomerase I and topoisomerase IIα. Molecular docking simulations suggested a different way in which the acridines 17a–17j can interact with topoisomerase I versus topoisomerase IIα. A strong correlation between the lipophilicity of the derivatives and their ability to stabilize the intercalation complex was identified for all of the studied agents. Acridines 17a–17j were also subjected to in vitro screening conducted by the Developmental Therapeutic Program of the National Cancer Institute (NCI) against a panel of 60 cancer cell lines. The strongest biological activity was displayed by aniline acridine 17a (MCF7–GI50 18.6 nM) and N,N-dimethylaniline acridine 17b (SR–GI50 38.0 nM). The relationship between the cytostatic activity of the most active substances (derivatives 17a, 17b, and 17e–17h) and their values of KB, LogP, ΔS°, and δ was also investigated. Due to the fact that a significant correlation was only found in the case of charge density, δ, it is possible to assume that the cytostatic effect might be dependent upon the structural specificity of the acridine derivatives." @default.
• W4318473113 created "2023-01-30" @default.
• W4318473113 creator A5006189027 @default.
• W4318473113 creator A5023109904 @default.
• W4318473113 creator A5031014102 @default.
• W4318473113 creator A5031419076 @default.
• W4318473113 creator A5075359249 @default.
• W4318473113 creator A5091205473 @default.
• W4318473113 date "2023-01-30" @default.
• W4318473113 modified "2023-09-25" @default.
• W4318473113 title "Novel 3,9-Disubstituted Acridines with Strong Inhibition Activity against Topoisomerase I: Synthesis, Biological Evaluation and Molecular Docking Study" @default.
• W4318473113 cites W129812222 @default.
• W4318473113 cites W1526205344 @default.
• W4318473113 cites W1819431423 @default.
• W4318473113 cites W1970409619 @default.
• W4318473113 cites W1982597534 @default.
• W4318473113 cites W1985982026 @default.
• W4318473113 cites W1990399577 @default.
• W4318473113 cites W1991739917 @default.
• W4318473113 cites W1994490060 @default.
• W4318473113 cites W2001856285 @default.
• W4318473113 cites W2005623502 @default.
• W4318473113 cites W2006853138 @default.
• W4318473113 cites W2010511880 @default.
• W4318473113 cites W2012703293 @default.
• W4318473113 cites W2022283419 @default.
• W4318473113 cites W2032084435 @default.
• W4318473113 cites W2038692006 @default.
• W4318473113 cites W2040203075 @default.
• W4318473113 cites W2045208351 @default.
• W4318473113 cites W2046229956 @default.
• W4318473113 cites W2046892466 @default.
• W4318473113 cites W2048187969 @default.
• W4318473113 cites W2057846793 @default.
• W4318473113 cites W2061163224 @default.
• W4318473113 cites W2068146209 @default.
• W4318473113 cites W2074134576 @default.
• W4318473113 cites W2113104789 @default.
• W4318473113 cites W2115127516 @default.
• W4318473113 cites W2132629607 @default.
• W4318473113 cites W2150788604 @default.
• W4318473113 cites W2158534713 @default.
• W4318473113 cites W2162569125 @default.
• W4318473113 cites W2165526004 @default.
• W4318473113 cites W2182237070 @default.
• W4318473113 cites W2236136189 @default.
• W4318473113 cites W2318025780 @default.
• W4318473113 cites W2400489255 @default.
• W4318473113 cites W2404280981 @default.
• W4318473113 cites W2563668542 @default.
• W4318473113 cites W2582222482 @default.
• W4318473113 cites W2745502933 @default.
• W4318473113 cites W2781930396 @default.
• W4318473113 cites W3101416967 @default.
• W4318473113 cites W3121640577 @default.
• W4318473113 cites W3187924265 @default.
• W4318473113 doi "https://doi.org/10.3390/molecules28031308" @default.
• W4318473113 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36770975" @default.
• W4318473113 hasPublicationYear "2023" @default.
• W4318473113 type Work @default.
• W4318473113 citedByCount "0" @default.
• W4318473113 crossrefType "journal-article" @default.
• W4318473113 hasAuthorship W4318473113A5006189027 @default.
• W4318473113 hasAuthorship W4318473113A5023109904 @default.
• W4318473113 hasAuthorship W4318473113A5031014102 @default.
• W4318473113 hasAuthorship W4318473113A5031419076 @default.
• W4318473113 hasAuthorship W4318473113A5075359249 @default.
• W4318473113 hasAuthorship W4318473113A5091205473 @default.
• W4318473113 hasBestOaLocation W43184731131 @default.
• W4318473113 hasConcept C116073593 @default.
• W4318473113 hasConcept C133571119 @default.
• W4318473113 hasConcept C137824038 @default.
• W4318473113 hasConcept C147897179 @default.
• W4318473113 hasConcept C159110408 @default.
• W4318473113 hasConcept C178790620 @default.
• W4318473113 hasConcept C185592680 @default.
• W4318473113 hasConcept C190283241 @default.
• W4318473113 hasConcept C202751555 @default.
• W4318473113 hasConcept C21951064 @default.
• W4318473113 hasConcept C2776924795 @default.
• W4318473113 hasConcept C2779102032 @default.
• W4318473113 hasConcept C2780500152 @default.
• W4318473113 hasConcept C2910410043 @default.
• W4318473113 hasConcept C41685203 @default.
• W4318473113 hasConcept C552990157 @default.
• W4318473113 hasConcept C55493867 @default.
• W4318473113 hasConcept C71240020 @default.
• W4318473113 hasConcept C71924100 @default.
• W4318473113 hasConceptScore W4318473113C116073593 @default.
• W4318473113 hasConceptScore W4318473113C133571119 @default.
• W4318473113 hasConceptScore W4318473113C137824038 @default.
• W4318473113 hasConceptScore W4318473113C147897179 @default.
• W4318473113 hasConceptScore W4318473113C159110408 @default.
• W4318473113 hasConceptScore W4318473113C178790620 @default.
• W4318473113 hasConceptScore W4318473113C185592680 @default.
• W4318473113 hasConceptScore W4318473113C190283241 @default.
• W4318473113 hasConceptScore W4318473113C202751555 @default.
• W4318473113 hasConceptScore W4318473113C21951064 @default.

• next