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Anti-proliferative and anti-malarial activities of spiroisoxazoline analogues of artemisinin

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cris.lastimport.scopus2024-02-12T19:50:56Z
dc.abstract.enA series of spiroisoxazoline analogues of artemisinin was synthesized by employing 1,3-dipolar cycloaddition between various in situ generated nitrile oxides and artemisitene. All the synthesized compounds were tested for their anti-proliferative and anti-malarial activities. Among the compounds tested, compound 11a was found to be potent against the HCT-15 cancer cell line with IC 50 = 4.04 μM when compared to 5-fluorouracil (IC 50 = 35.53 μM). DNA cell cycle analysis shows that 11a was inhibiting cell proliferation at the G2/M phase. Compound 11b was found to be most active against Plasmodium falciparum with IC 50 = 0.1 μM and also blocked host hemoglobin hydrolysis by the falcipain-3 receptor. It was demonstrated to have better dynamics of parasite killing efficiency than artemisinin. Molecular docking studies revealed that these compounds interacted with falcipain-3 receptor sites.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorNaaz, Fatima
dc.contributor.authorNayakanti, Devanna
dc.contributor.authorKumar, Halmuthur M. S.
dc.contributor.authorAkhter, Mymoona
dc.contributor.authorPratap, Surya
dc.contributor.authorSahal, Dinakar
dc.contributor.authorShafi, Syed
dc.contributor.authorSharma, Kalicharan
dc.contributor.authorPandey, Kailash
dc.contributor.authorReddy, Srinivas
dc.contributor.authorKumari, Vandana
dc.contributor.authorJha, Kunal
dc.date.accessioned2024-01-24T16:40:36Z
dc.date.available2024-01-24T16:40:36Z
dc.date.issued2019
dc.description.financeNie dotyczy
dc.description.number1
dc.description.volume352
dc.identifier.doi10.1002/ARDP.201800192
dc.identifier.issn0365-6233
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/100806
dc.identifier.weblinkhttps://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1002%2Fardp.201800192
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofArchiv der Pharmazie
dc.relation.pagesart.no. 1800192
dc.rightsClosedAccess
dc.sciencecloudnosend
dc.subject.en1,3-dipolar cycloaddition
dc.subject.enanti-malarial activity
dc.subject.enanti-proliferative
dc.subject.enartemisitene
dc.subject.enspiroisoxazoline
dc.titleAnti-proliferative and anti-malarial activities of spiroisoxazoline analogues of artemisinin
dc.typeJournalArticle
dspace.entity.typePublication