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Dostęp zamkniętyDesign, synthesis and biological evaluation of novel 2-alkylidene 19-norcalcitriol analogs.
| cris.lastimport.scopus | 2024-02-12T20:42:30Z |
| dc.abstract.en | Continuing our studies aimed at A-ring modified vitamin D compounds, we designed novel 19-norcalcitriol derivatives bearing at C-2 pegylated chains of different lengths. The terminal fragments of these substituents contain hydroxyls or moieties possessing nitrogen and/or sulfur atoms capable of transition metal ions complexation. Also, two conjugate–type platinum(II) complexes of 19-norcalcitriol were obtained in which l-methionine served as chelating moiety. The convergent synthesis of the target 19-norcalcitriol analogs involved several steps with the crucial one being condensation of A-ring phosphine oxide and the known Grundmann ketone by Wittig-Horner reaction. Further elaboration of the 2-alkylidene substituent provided all final compounds which were then tested to determine their affinity for the vitamin D receptor and cytotoxic activity. |
| dc.affiliation | Uniwersytet Warszawski |
| dc.contributor.author | Berkowska, Klaudia |
| dc.contributor.author | Siciński, Rafał |
| dc.contributor.author | Marcinkowska, Ewa |
| dc.contributor.author | Rárová, Lucie |
| dc.contributor.author | Fabisiak, Adrian |
| dc.contributor.author | Brzemiński, Paweł |
| dc.date.accessioned | 2024-01-24T21:35:47Z |
| dc.date.available | 2024-01-24T21:35:47Z |
| dc.date.issued | 2020 |
| dc.description.finance | Publikacja bezkosztowa |
| dc.description.volume | 101 |
| dc.identifier.doi | 10.1016/J.BIOORG.2020.104013 |
| dc.identifier.issn | 0045-2068 |
| dc.identifier.uri | https://repozytorium.uw.edu.pl//handle/item/104613 |
| dc.identifier.weblink | http://doi.org/10.1016/j.bioorg.2020.104013 |
| dc.language | eng |
| dc.pbn.affiliation | chemical sciences |
| dc.relation.ispartof | Bioorganic Chemistry |
| dc.relation.pages | 1-14 |
| dc.rights | ClosedAccess |
| dc.sciencecloud | nosend |
| dc.subject.en | 19-Norcalcitriol |
| dc.subject.en | Vitamin D receptor |
| dc.subject.en | Wittig-Horner reaction |
| dc.subject.en | Platinum(II) complexes |
| dc.subject.en | Drug delivery systems |
| dc.title | Design, synthesis and biological evaluation of novel 2-alkylidene 19-norcalcitriol analogs. |
| dc.type | JournalArticle |
| dspace.entity.type | Publication |