DC pole | Wartość | Język |
dc.contributor.author | Adamus-Grabicka, Angelika A. | - |
dc.contributor.author | Markowicz-Piasecka, Magdalena | - |
dc.contributor.author | Cieślak, Marcin | - |
dc.contributor.author | Królewska-Golińska, Karolina | - |
dc.contributor.author | Hikisz, Paweł | - |
dc.contributor.author | Kusz, Joachim | - |
dc.contributor.author | Małecka, Magdalena | - |
dc.contributor.author | Budzisz, Elżbieta | - |
dc.date.accessioned | 2020-04-03T08:21:34Z | - |
dc.date.available | 2020-04-03T08:21:34Z | - |
dc.date.issued | 2020 | - |
dc.identifier.citation | "Molecules" Vol. 25, iss. 7 (2020), art. no 1613 | pl_PL |
dc.identifier.issn | 1420-3049 | - |
dc.identifier.uri | http://hdl.handle.net/20.500.12128/13431 | - |
dc.description.abstract | A series of 3-benzylidenechrmanones 1, 3, 5, 7, 9 and their spiropyrazoline analogues 2, 4, 6, 8,
10were synthesized. X-ray analysis confirms that compounds 2 and 8 crystallize in amonoclinic system
in P21/n space groups with one and three molecules in each asymmetric unit. The crystal lattice of the
analyzed compounds is enhanced by hydrogen bonds. The primary aim of the study was to evaluate
the anti-proliferative potential of 3-benzylidenechromanones and their spiropyrazoline analogues
towards four cancer cell lines. Our results indicate that parent compounds 1 and 9 with a phenyl ring
at C2 have lower cytotoxic activity against cancer cell lines than their spiropyrazolines analogues.
Analysis of IC50 values showed that the compounds 3 and 7 exhibited higher cytotoxic activity against
cancer cells, being more active than the reference compound (4-chromanone or quercetin). The results
of this study indicate that the incorporation of a pyrazoline ring into the 3-arylideneflavanone results
in an improvement of the compounds’ activity and therefore it may be of use in the search of new
anticancer agents. Further analysis allowed us to demonstrate the compounds to have a strong
inhibitory effect on the cell cycle. For instance, compounds 2, 10 induced 60% of HL-60 cells to be
arrested in G2/M phase. Using a DNA-cleavage protection assay we also demonstrated that tested
compounds interact with DNA. All compounds at the concentrations corresponding to cytotoxic
properties are not toxic towards red blood cells, and do not contribute to hemolysis of RBCs. | pl_PL |
dc.language.iso | en | pl_PL |
dc.rights | Uznanie autorstwa 3.0 Polska | * |
dc.rights.uri | http://creativecommons.org/licenses/by/3.0/pl/ | * |
dc.subject | 3-benzylideneflavanone/3-benzylidenechromanone | pl_PL |
dc.subject | spiropyrazolines | pl_PL |
dc.subject | cytotoxicity | pl_PL |
dc.subject | lipophilicity | pl_PL |
dc.subject | DNA interaction | pl_PL |
dc.title | Biological Evaluation of 3-Benzylidenechromanones and Their Spiropyrazolines-Based Analogues | pl_PL |
dc.type | info:eu-repo/semantics/article | pl_PL |
dc.identifier.doi | 10.3390/molecules25071613 | - |
Pojawia się w kolekcji: | Artykuły (WNŚiT)
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