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Verubulin (Azixa) Analogues with Increased Saturation: Synthesis, SAR and Encapsulation in Biocompatible Nanocontainers Based on Ca2+ or Mg2+ Cross-Linked Alginate

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dc.contributor.authorSedenkova, K. N.
dc.contributor.authorLeschukov, D. N.
dc.contributor.authorGrishin, Y. K.
dc.contributor.authorZefirov, N. A.
dc.contributor.authorShtil, A. A.
dc.contributor.authorШтиль, Александр Альбертович
dc.date.accessioned2024-12-27T11:03:44Z
dc.date.available2024-12-27T11:03:44Z
dc.date.issued2023
dc.description.abstractTubulin-targeting agents attract undiminished attention as promising compounds for the design of anti-cancer drugs. Verubulin is a potent tubulin polymerization inhibitor, binding to colchicine-binding sites. In the present work, a series of verubulin analogues containing a cyclohexane or cycloheptane ring 1,2-annulated with pyrimidine moiety and various substituents in positions 2 and 4 of pyrimidine were obtained and their cytotoxicity towards cancer and non-cancerous cell lines was estimated. The investigated compounds revealed activity against various cancer cell lines with IC50 down to 1–4 nM. According to fluorescent microscopy data, compounds that showed cytotoxicity in the MTT test disrupt the normal cytoskeleton of the cell in a pattern similar to that for combretastatin A-4. The hit compound (N-(4-methoxyphenyl)-N,2-dimethyl-5,6,7,8-tetrahydroquinazolin-4-amine) was encapsulated in biocompatible nanocontainers based on Ca2+ or Mg2+ cross-linked alginate and it was demonstrated that its cytotoxic activity was preserved after encapsulation.
dc.identifier.citationVerubulin (Azixa) Analogues with Increased Saturation: Synthesis, SAR and Encapsulation in Biocompatible Nanocontainers Based on Ca2+ or Mg2+ Cross-Linked Alginate / Sedenkova, K. N. [et al.] // Pharmaceuticals. - 2023. - 16. - № 10. - 10.3390/ph16101499
dc.identifier.doi10.3390/ph16101499
dc.identifier.urihttps://www.doi.org/10.3390/ph16101499
dc.identifier.urihttps://www.scopus.com/record/display.uri?eid=2-s2.0-85175454958&origin=resultslist
dc.identifier.urihttps://openrepository.mephi.ru/handle/123456789/29391
dc.relation.ispartofPharmaceuticals
dc.subjectMoiety
dc.subjectMTT assay
dc.subjectRuthenium Catalysts
dc.titleVerubulin (Azixa) Analogues with Increased Saturation: Synthesis, SAR and Encapsulation in Biocompatible Nanocontainers Based on Ca2+ or Mg2+ Cross-Linked Alginate
dc.typeArticle
dspace.entity.typePublication
oaire.citation.issue10
oaire.citation.volume16
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relation.isAuthorOfPublication.latestForDiscoveryd2e4a764-d93d-47f5-a8bc-09f718b121f7
relation.isOrgUnitOfPublication010157d0-1f75-46b2-ab5b-712e3424b4f5
relation.isOrgUnitOfPublication.latestForDiscovery010157d0-1f75-46b2-ab5b-712e3424b4f5
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