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dc.contributor.authorHåheim, Katja Stangeland
dc.contributor.authorLindback, Emil
dc.contributor.authorTan, Kah Ni
dc.contributor.authorAlbrigtsen, Marte
dc.contributor.authorHelgeland, Ida Therese Urdal
dc.contributor.authorClemence, Lauga
dc.contributor.authorMatringe, Theodora
dc.contributor.authorKennedy, Emily K.
dc.contributor.authorAndersen, Jeanette Hammer
dc.contributor.authorAvery, Vicky M.
dc.contributor.authorSydnes, Magne Olav
dc.date.accessioned2021-06-21T20:51:14Z
dc.date.available2021-06-21T20:51:14Z
dc.date.issued2021-05-30
dc.description.abstractA series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts 10 and 21 showed the most promising antiplasmodial inhibition, with compound 10 displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine 4b to be significantly more active against human prostate cancer (IC<sub>50</sub> = 24 nM) than Puromycin (IC<sub>50</sub> = 270 nM) and Doxorubicin (IC<sub>50</sub> = 830 nM), which are used for clinical treatment. Pyridocarbazoles 9 was also moderately effective against all the employed cancer cell lines and moreover showed excellent biofilm inhibition (9a: MBIC = 100 µM; 9b: MBIC = 100 µM).en_US
dc.identifier.citationHåheim KS, Lindback E, Tan, Albrigtsen M, Helgeland IT, Clemence, Matringe, Kennedy, Andersen JH, Avery, Sydnes MO. Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioiso-Mers for Antimalarial, Antiproliferative and Antimicrobial Activities. Molecules. 2021;26en_US
dc.identifier.cristinIDFRIDAID 1912694
dc.identifier.doi10.3390/molecules26113268
dc.identifier.issn1420-3049
dc.identifier.urihttps://hdl.handle.net/10037/21500
dc.language.isoengen_US
dc.publisherMDPIen_US
dc.relation.journalMolecules
dc.rights.accessRightsopenAccessen_US
dc.rights.holderCopyright 2021 The Author(s)en_US
dc.subjectVDP::Mathematics and natural science: 400::Chemistry: 440::Pharmaceutical chemistry: 448en_US
dc.subjectVDP::Matematikk og Naturvitenskap: 400::Kjemi: 440::Legemiddelkjemi: 448en_US
dc.titleSynthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioiso-Mers for Antimalarial, Antiproliferative and Antimicrobial Activitiesen_US
dc.type.versionpublishedVersionen_US
dc.typeJournal articleen_US
dc.typeTidsskriftartikkelen_US
dc.typePeer revieweden_US


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