Novel diarylamides and diarylureas with N-substitution dependent activity against medulloblastoma

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dc.cclicenceCC-BY-NC-NDen
dc.contributor.authorSnape, Timothy J.
dc.contributor.authorLawson, Christopher
dc.contributor.authorAlta, Thowaiba Babikr Ahmed
dc.contributor.authorMoschou, Georgia
dc.contributor.authorSkamnaki, Vasiliki
dc.contributor.authorSolovou, Theodora G. A.
dc.contributor.authorTopham, Caroline
dc.contributor.authorHayes, Joseph
dc.date.acceptance2021-08-05
dc.date.accessioned2021-08-14T09:09:14Z
dc.date.available2021-08-14T09:09:14Z
dc.date.issued2021-08-09
dc.descriptionThe file attached to this record is the author's final peer reviewed version. The Publisher's final version can be found by following the DOI link.en
dc.description.abstractMedulloblastoma – highly aggressive and heterogeneous tumours of the cerebellum – account for 15-20% of all childhood brain tumours, and are the most common high-grade childhood embryonal tumour of the central nervous system. Herein, potent in vitro anticancer activity against two established medulloblastoma cell lines of the sonic hedgehog subgroup, namely DAOY (p53 mutant) and ONS-76 (p53 wild type), has been achieved. A number of first-generation diarylamides and diarylureas were evaluated and activity is likely to be, in-part, conformation-dependent. The most active compound from this first-generation set of compounds, 1-naphthyl derivative 4b, was selected and a second-generation of compounds were optimised and tested for activity against the medulloblastoma cell lines. This process resulted in drug-like compounds with up to sixty times the activity (sub-micromolar) of the first-generation – thus providing potent new leads for further study.en
dc.funderNo external funderen
dc.identifier.citationSnape, T.J., Lawson, C., Alta, T.B.A., Moschou, G., Skamnaki, V., Solovou, T.G.A., Topham, C., Hayes, J. (2021) Novel diarylamides and diarylureas with N-substitution dependent activity against medulloblastoma. European Journal of Medicinal Chemistry, 225, 113751.en
dc.identifier.doihttps://doi.org/10.1016/j.ejmech.2021.113751
dc.identifier.issn0223-5234
dc.identifier.urihttps://dora.dmu.ac.uk/handle/2086/21188
dc.language.isoenen
dc.peerreviewedYesen
dc.publisherElsevieren
dc.researchinstituteLeicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)en
dc.titleNovel diarylamides and diarylureas with N-substitution dependent activity against medulloblastomaen
dc.typeArticleen

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