Aminobenzofuran-containing analogues of proximicins exhibit higher antiproliferative activity against human UG-87 glioblastoma cells compared to temozolomide

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dc.cclicenceCC BYen
dc.contributor.authorShokrzadeh Madieh, Nasrin
dc.contributor.authorBrucoli, Federico
dc.contributor.authorTanna, Sangeeta
dc.contributor.authorAlqurayn, Norah Ahmed
dc.contributor.authorVaideanu, Alexandra
dc.contributor.authorSchatzlein, Andreas
dc.date.accessioned2023-04-25T14:31:43Z
dc.date.available2023-04-25T14:31:43Z
dc.date.issued2023-03-14
dc.descriptionopen access articleen
dc.description.abstractA new series of proximicin analogues containing a benzofuran moiety as the replacement of the di-furan scaffold of the parent compound were synthesised and evaluated for their anti-proliferative activities against human glioblastoma cells U-87 MG. Proximicins A, B, and C are secondary metabolites produced by Verrucosispora Fiedleri MG-37, a Gram-positive actinomycete isolated from deep-sea sediment. Proximicins exhibit significant cytotoxic and apoptotic effects in a number of tumour cell lines, although further investigations on these natural products biological activity are hampered by the challenging synthesis of their constitutive di-furan unit. Therefore, the easily-synthesisable benzofuran ring was elected as a replacement of the di-furan platform, and a library of proximicin analogues was prepared in which different substituents were introduced at both the N-terminus and C-terminus of the benzofuran core unit. The novel compounds were tested against U-87 MG, as it was previously found that proximicins targeted this cancerous cell line, and the human healthy cell line WI-38. Temozolomide, the chemotherapeutic agent of choice for the treatment of glioblastoma, was used as a control. Analysis of growth inhibitory concentration values revealed that a number of furan-benzofuran-containing proximicin analogues, including 23(16) (IC50 U-87 MG = 6.54 μg mL−1) exhibited higher antiproliferative activity against glioblastoma cells compared to both proximicins A–C and temozolomide (IC50 U-87 MG = 29.19 μg mL−1) in U-87 MG.en
dc.funderNo external funderen
dc.identifier.citationShokrzadeh Madieh, N. et al. (2023) Aminobenzofuran-containing analogues of proximicins exhibit higher antiproliferative activity against human UG-87 glioblastoma cells compared to temozolomide. RSC Advances, 13, pp. 8420-8426en
dc.identifier.doihttps://doi.org/10.1039/D3RA00107E
dc.identifier.urihttps://hdl.handle.net/2086/22756
dc.language.isoenen
dc.peerreviewedYesen
dc.publisherRoyal Society of Chemistryen
dc.researchinstituteLeicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)en
dc.titleAminobenzofuran-containing analogues of proximicins exhibit higher antiproliferative activity against human UG-87 glioblastoma cells compared to temozolomideen
dc.typeArticleen

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